Topotecan (Synonyms: SKF 104864A; NSC 609669)

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Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Topotecan hydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

Topotecan Chemical Structure

CAS No. : 123948-87-8

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Other In-stock Forms of Topotecan:

Topotecan hydrochloride

Other Forms of Topotecan:

Topotecan hydrochloride In-stock
Topotecan-d5 Get quote
Topotecan-d₆ Get quote
Topotecan hydrochloride hydrate Get quote

26 Publications Citing Use of MCE Topotecan

: Topotecan purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 21;10(1):3761. [Abstract]; WDR5 inhibitor OICR-9429 enhances the sensitivity of ovarian cancer to genotoxic chemotherapeutics in vivo. Representative images and the apoptotic rate the indicated chemotherapy-treated xenograft tumors.

: Topotecan purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 21;10(1):3761. [Abstract]; IB analysis of the level of cleaved-caspase 3 and cleaved-PARP1 in the indicated chemotherapy-treated xenograft tumors. GAPDH served as the loading control.

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Topoisomerase Topo I Topo II

Biological Activity
Protocol
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

Topoisomerase I

Cellular Effect

Cell Line	Type	Value	Description	References
2008	IC₅₀	> 500 nM Compound: 2	Antiproliferative activity against human 2008 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human 2008 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35932565]
A2780	IC₅₀	0.006 μM Compound: 4	Cytotoxicity against human A2780 cells overexpressing alpha5beta3 integrin assessed as cell survival after 72 hrs by SRB assay Cytotoxicity against human A2780 cells overexpressing alpha5beta3 integrin assessed as cell survival after 72 hrs by SRB assay	[PMID: 22959246]
A2780	IC₅₀	0.078 μM Compound: 2; TPT	Antiproliferative activity against human A2780 cells after 96 hrs by MTT assay Antiproliferative activity against human A2780 cells after 96 hrs by MTT assay	[PMID: 27871039]
A2780	IC₅₀	1.1 μM Compound: Topotecan	Cytotoxicity against human A2780 cells after 96 hrs by MTT assay Cytotoxicity against human A2780 cells after 96 hrs by MTT assay	[PMID: 16792409]
A2780	IC₅₀	1.2 μM Compound: Topotecan	Cytotoxicity against human A2780 cells after 96 hrs by MTT assay Cytotoxicity against human A2780 cells after 96 hrs by MTT assay	[PMID: 17125236]
A2780	IC₅₀	22 μM Compound: Topotecan	Potentiation of growth inhibition of A2780 cells by compound alone in experiment 2 Potentiation of growth inhibition of A2780 cells by compound alone in experiment 2	[PMID: 11063605]
A2780	IC₅₀	22.6 μM Compound: Topotecan	Potentiation of growth inhibition of A2780 cells by compound alone in experiment 1 Potentiation of growth inhibition of A2780 cells by compound alone in experiment 1	[PMID: 11063605]
A2780	IC₅₀	3.35 μM Compound: 2, TPT	Cytotoxicity against human A2780 cells after 4 days by MTT assay Cytotoxicity against human A2780 cells after 4 days by MTT assay	[PMID: 18554906]
A2780	IC₅₀	33 nM Compound: Topotecan	Cytotoxicity against human A2780 cells after 72 hrs by MTT assay Cytotoxicity against human A2780 cells after 72 hrs by MTT assay	[PMID: 24900725]
A-375	IC₅₀	13 nM Compound: 7	Cytotoxicity against human A375 cells after 72 hrs by alamar blue assay Cytotoxicity against human A375 cells after 72 hrs by alamar blue assay	[PMID: 21341674]
A498	IC₅₀	2 μM Compound: Topotecan	Inhibition of colony formation of human A498 cells after 2 weeks by crystal violet staining-based microscopic analysis Inhibition of colony formation of human A498 cells after 2 weeks by crystal violet staining-based microscopic analysis	[PMID: 29993250]
A549	IC₅₀	0.0032 μM Compound: topotecan	Cytotoxicity against human A549 cells after 96 hrs by MTT assay Cytotoxicity against human A549 cells after 96 hrs by MTT assay	[PMID: 15165144]
A549	IC₅₀	0.005 μM Compound: topotecan, TPT	Antitumor activity against human A549 cells after 4 hrs by MTT assay Antitumor activity against human A549 cells after 4 hrs by MTT assay	[PMID: 18207748]
A549	IC₅₀	0.007 μM Compound: 2; TPT	Antiproliferative activity against human A549 cells after 96 hrs by MTT assay Antiproliferative activity against human A549 cells after 96 hrs by MTT assay	[PMID: 27871039]
A549	IC₅₀	0.04 μM Compound: 2, Hycamtin	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 20371183]
A549	IC₅₀	0.045 μM Compound: 2	Cytotoxicity against human A549 cells after 72 hrs by SRB assay Cytotoxicity against human A549 cells after 72 hrs by SRB assay	[PMID: 25438769]
A549	IC₅₀	0.0452 μM Compound: 2	Cytotoxicity against human A549 cells after 72 hrs sulforhodamine B colorimetric assay Cytotoxicity against human A549 cells after 72 hrs sulforhodamine B colorimetric assay	[PMID: 25008456]
A549	IC₅₀	0.071 μM Compound: 2, TPT	Cytotoxicity against human A549 cells after 3 days Cytotoxicity against human A549 cells after 3 days	[PMID: 21333532]
A549	IC₅₀	0.11 μM Compound: 3; TPT	Cytotoxicity against human A549 cells after 72 hrs by SRB assay Cytotoxicity against human A549 cells after 72 hrs by SRB assay	[PMID: 28789891]
A549	IC₅₀	0.2 μM Compound: TPT	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 26725027]
A549	IC₅₀	0.22 μM Compound: 2, TPT	Cytotoxicity against human A549 cells after 4 days by MTT assay Cytotoxicity against human A549 cells after 4 days by MTT assay	[PMID: 18554906]
A549	IC₅₀	0.36 μM Compound: 3	Antitumor activity against human A549/ATCC cells by SRB method Antitumor activity against human A549/ATCC cells by SRB method	[PMID: 19541483]
A549	IC₅₀	0.48 μM Compound: Topotecan	Cytotoxicity against human A549 cells by SRB method Cytotoxicity against human A549 cells by SRB method	[PMID: 18986807]
A549	GI₅₀	0.9 μM Compound: 3, TPT	Cytotoxicity against human A549 cells expressing wild type p53 after 48 hrs by SRB assay Cytotoxicity against human A549 cells expressing wild type p53 after 48 hrs by SRB assay	[PMID: 19715319]
A549	IC₅₀	1.09 μM Compound: Topotecan	Cytotoxicity against human A549 cells after 3 days by MTT assay Cytotoxicity against human A549 cells after 3 days by MTT assay	[PMID: 20202723]
A549	IC₅₀	1.11 μM Compound: TPT	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 34990980]
A549	IC₅₀	1.424 μM Compound: Topotecan	Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 30227711]
A549	IC₅₀	1.9 μM Compound: 3, TPT	Cytotoxicity against human A549 cells expressing wild type p53 after 48 hrs by SRB assay Cytotoxicity against human A549 cells expressing wild type p53 after 48 hrs by SRB assay	[PMID: 19715319]
A549	IC₅₀	112 nM Compound: 3	Cytotoxicity against human A549 cells after 72 hrs by SRB assay Cytotoxicity against human A549 cells after 72 hrs by SRB assay	[PMID: 28927790]
A549	IC₅₀	112 nM Compound: 3	Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay	[PMID: 28285912]
A549	IC₅₀	2.8 μM Compound: TPT	Antiproliferative activity against human A549 cells after 3 days by MTT assay Antiproliferative activity against human A549 cells after 3 days by MTT assay	[PMID: 23084702]
A549	IC₅₀	24 nM Compound: Topotecan	Cytotoxic potentiation of Topotecan (TP) by the compound in human lung carcinoma A549 cell line Cytotoxic potentiation of Topotecan (TP) by the compound in human lung carcinoma A549 cell line	[PMID: 12408707]
A549	IC₅₀	3.16 μM Compound: TPT, Hycamptin	Cytotoxicity against human A549 cells after 3 days by MTT assay Cytotoxicity against human A549 cells after 3 days by MTT assay	[PMID: 21463912]
A549	IC₅₀	3.3 μM Compound: Topotecan	Cytotoxicity against human A549 cells after 96 hrs by MTT assay Cytotoxicity against human A549 cells after 96 hrs by MTT assay	[PMID: 16792409]
A549	IC₅₀	3.5 μM Compound: Topotecan	Cytotoxicity against human A549 cells after 96 hrs by MTT assay Cytotoxicity against human A549 cells after 96 hrs by MTT assay	[PMID: 17125236]
A549	GI₅₀	3.96 μM Compound: TPT	Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 22867019]
A549	IC₅₀	354 nM Compound: Topotecan	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 24900725]
A549	IC₅₀	4.81 μM Compound: Topotecan	Antiproliferative activity against human A549 cells after 3 days by XTT assay Antiproliferative activity against human A549 cells after 3 days by XTT assay	[PMID: 24727241]
A549	IC₅₀	4.81 μM Compound: Top	Antiproliferative activity against human A549 cells after 72 hrs by XTT assay Antiproliferative activity against human A549 cells after 72 hrs by XTT assay	[PMID: 23237975]
A549	GI₅₀	5.98 μM Compound: Topotecan	Growth inhibition of human A549 cells after 72 hrs by XTT assay Growth inhibition of human A549 cells after 72 hrs by XTT assay	[PMID: 22079254]
A549	GI₅₀	5.98 μM Compound: Topotecan	Antiproliferative activity against human A549 cells after 72 hrs by XTT assay Antiproliferative activity against human A549 cells after 72 hrs by XTT assay	[PMID: 19796956]
A549	IC₅₀	58.4 nM Compound: Topotecan	Cytotoxicity against human A549 cells assessed as growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as growth inhibition measured after 72 hrs by MTT assay	[PMID: 31881457]
A549	IC₅₀	7.4 μM Compound: TPT	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 26226379]
A549	IC₅₀	8.3 μM Compound: Topotecan	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay	[PMID: 35238576]
AGS	GI₅₀	0.1 μM Compound: 3, TPT	Cytotoxicity against human AGS cells expressing wild type p53 after 48 hrs by SRB assay Cytotoxicity against human AGS cells expressing wild type p53 after 48 hrs by SRB assay	[PMID: 19715319]
AGS	IC₅₀	0.3 μM Compound: 3, TPT	Cytotoxicity against human AGS cells expressing wild type p53 after 48 hrs by SRB assay Cytotoxicity against human AGS cells expressing wild type p53 after 48 hrs by SRB assay	[PMID: 19715319]
Astrocyte	IC₅₀	0.16 μM Compound: Topotecan	Cytotoxicity against normal human astrocytes assessed as cell viability incubated for 72 hrs by WST-1 method Cytotoxicity against normal human astrocytes assessed as cell viability incubated for 72 hrs by WST-1 method	[PMID: 26355532]
Bel-7402	IC₅₀	0.0012 μM Compound: topotecan	Cytotoxicity against human Bel7402 cells after 96 hrs by MTT assay Cytotoxicity against human Bel7402 cells after 96 hrs by MTT assay	[PMID: 15165144]
Bel-7402	IC₅₀	0.1 μM Compound: 2; TPT	Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay	[PMID: 27871039]
Bel-7402	IC₅₀	0.47 μM Compound: 2, TPT	Cytotoxicity against human Bel7402 cells after 3 days Cytotoxicity against human Bel7402 cells after 3 days	[PMID: 21333532]
Bel-7402	IC₅₀	1.2 μM Compound: Topotecan	Cytotoxicity against human Bel7402 cells after 96 hrs by MTT assay Cytotoxicity against human Bel7402 cells after 96 hrs by MTT assay	[PMID: 16792409]
Bel-7402	IC₅₀	1.4 μM Compound: Topotecan	Cytotoxicity against human Bel-7402 cells after 96 hrs by MTT assay Cytotoxicity against human Bel-7402 cells after 96 hrs by MTT assay	[PMID: 17125236]
Bel-7402	IC₅₀	3.13 μM Compound: 2, TPT	Cytotoxicity against human BEL-7402 cells after 4 days by MTT assay Cytotoxicity against human BEL-7402 cells after 4 days by MTT assay	[PMID: 18554906]
Bel-7402	IC₅₀	7.118 μM Compound: Topotecan	Cytotoxicity in human Bel7402 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human Bel7402 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 30227711]
BGC-823	IC₅₀	0.0043 μM Compound: topotecan	Cytotoxicity against human BGC823 cells after 96 hrs by MTT assay Cytotoxicity against human BGC823 cells after 96 hrs by MTT assay	[PMID: 15165144]
BGC-823	IC₅₀	0.078 μM Compound: 2; TPT	Antiproliferative activity against human BGC823 cells after 96 hrs by MTT assay Antiproliferative activity against human BGC823 cells after 96 hrs by MTT assay	[PMID: 27871039]
BGC-823	IC₅₀	3.8 μM Compound: Topotecan	Cytotoxicity against human BGC-823 cells after 96 hrs by MTT assay Cytotoxicity against human BGC-823 cells after 96 hrs by MTT assay	[PMID: 17125236]
BGC-823	IC₅₀	4.4 μM Compound: Topotecan	Cytotoxicity against human BGC823 cells after 96 hrs by MTT assay Cytotoxicity against human BGC823 cells after 96 hrs by MTT assay	[PMID: 16792409]
Bone marrow cell	IC₅₀	130 nM Compound: 7	Cytotoxicity against human bone marrow cell by CFU-GM assay Cytotoxicity against human bone marrow cell by CFU-GM assay	[PMID: 21341674]
Bone marrow cell	IC₅₀	8 nM Compound: 7	Cytotoxicity against mouse bone marrow cell by CFU-GM assay Cytotoxicity against mouse bone marrow cell by CFU-GM assay	[PMID: 21341674]
BXPC-3	IC₅₀	0.62 μM Compound: 2, TPT	Cytotoxicity against human BXPC3 cells after 4 days by MTT assay Cytotoxicity against human BXPC3 cells after 4 days by MTT assay	[PMID: 18554906]
C6	IC₅₀	5.8 μM Compound: Topotecan	Antiproliferative activity against rat C6 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against rat C6 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 34537445]
COR-L23	IC₅₀	13.2 nM Compound: Topotecan	Cytotoxicity measured using the COR-L23 parental (COR-L23/P) human non small cell lung carcinoma cell line Cytotoxicity measured using the COR-L23 parental (COR-L23/P) human non small cell lung carcinoma cell line	[PMID: 11806724]
DU-145	GI₅₀	0.01 μM Compound: 2	Growth inhibition of human DU145 cells by five-dose growth inhibition assay Growth inhibition of human DU145 cells by five-dose growth inhibition assay	[PMID: 25909279]
DU-145	IC₅₀	1.2 μM Compound: Topotecan	Antiproliferative activity against human DU145 cells by [3H]thymidine incorporation assay Antiproliferative activity against human DU145 cells by [3H]thymidine incorporation assay	[PMID: 20932758]
DU-145	IC₅₀	1000 nM Compound: 7	Cytotoxicity against human DU145 cells after 72 hrs by alamar blue assay Cytotoxicity against human DU145 cells after 72 hrs by alamar blue assay	[PMID: 21341674]
GES1	IC₅₀	6.22 μM Compound: TPT	Antiproliferative activity against human GES1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human GES1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 34990980]
GES1	IC₅₀	8.55 μM Compound: TPT	Antiproliferative activity against human GES1 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human GES1 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34774339]
H69AR	IC₅₀	> 300 nM Compound: 7	Cytotoxicity against human H69AR cells overexpressing MDR1 after 72 hrs by alamar blue assay Cytotoxicity against human H69AR cells overexpressing MDR1 after 72 hrs by alamar blue assay	[PMID: 21341674]
HCT-116	GI₅₀	0.03 μM Compound: 2	Growth inhibition of human HCT116 cells by five-dose growth inhibition assay Growth inhibition of human HCT116 cells by five-dose growth inhibition assay	[PMID: 25909279]
HCT-116	IC₅₀	0.0889 μM Compound: TPT	Antiproliferative activity against human HCT116 cells after 3 days by MTT assay Antiproliferative activity against human HCT116 cells after 3 days by MTT assay	[PMID: 23084702]
HCT-116	GI₅₀	0.4 μM Compound: TPT	Cytotoxicity against human HCT116 cells incubated for 72 hrs by MTT assay Cytotoxicity against human HCT116 cells incubated for 72 hrs by MTT assay	[PMID: 22867019]
HCT-116	IC₅₀	0.7 μM Compound: TPT	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 26226379]
HCT-116	IC₅₀	0.97 μM Compound: Topotecan	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay	[PMID: 35238576]
HCT-116	IC₅₀	1.1 μM Compound: TPT, Hycamptin	Cytotoxicity against human HCT116 cells after 3 days by MTT assay Cytotoxicity against human HCT116 cells after 3 days by MTT assay	[PMID: 21463912]
HCT-116	IC₅₀	4.32 μM Compound: TPT	Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 24826818]
HCT-116	IC₅₀	70.35 μM Compound: TPT	Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 26725027]
HCT-8	IC₅₀	0.0015 μM Compound: topotecan	Cytotoxicity against human HCT8 cells after 96 hrs by MTT assay Cytotoxicity against human HCT8 cells after 96 hrs by MTT assay	[PMID: 15165144]
HCT-8	IC₅₀	0.022 μM Compound: 2; TPT	Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay	[PMID: 27871039]
HCT-8	IC₅₀	0.07 μM Compound: Topotecan	Cytotoxicity against human HCT8 cells after 3 days by MTT assay Cytotoxicity against human HCT8 cells after 3 days by MTT assay	[PMID: 20392545]
HCT-8	IC₅₀	1.2 μM Compound: Topotecan	Cytotoxicity against human HCT8 cells after 96 hrs by MTT assay Cytotoxicity against human HCT8 cells after 96 hrs by MTT assay	[PMID: 17125236]
HCT-8	IC₅₀	1.5 μM Compound: Topotecan	Cytotoxicity against human HCT8 cells after 96 hrs by MTT assay Cytotoxicity against human HCT8 cells after 96 hrs by MTT assay	[PMID: 16792409]
HCT-8	IC₅₀	3.66 μM Compound: 2, TPT	Cytotoxicity against human HCT8 cells by MTT assay Cytotoxicity against human HCT8 cells by MTT assay	[PMID: 19056266]
HEK293	IC₅₀	1.3 μM Compound: topotecan	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	61 μM Compound: topotecan	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	8.6 μM Compound: topotecan	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEL	IC₅₀	26 μM Compound: Topotecan	Antiproliferative activity against HEL cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay Antiproliferative activity against HEL cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay	[PMID: 35238576]
HeLa	GI₅₀	0.03 μM Compound: topotecan	Growth inhibition of HeLa cells after 4 days Growth inhibition of HeLa cells after 4 days	[PMID: 17418582]
HeLa	GI₅₀	0.08 μM Compound: 3, TPT	Cytotoxicity against p53-deficient human HeLa cells after 48 hrs by SRB assay Cytotoxicity against p53-deficient human HeLa cells after 48 hrs by SRB assay	[PMID: 19715319]
HeLa	IC₅₀	0.73 μM Compound: Topotecan	Inhibition of DNA topoisomerase 2 in human HeLa cells incubated for 18 to 24 hrs by kinase assay Inhibition of DNA topoisomerase 2 in human HeLa cells incubated for 18 to 24 hrs by kinase assay	[PMID: 31416740]
HeLa	IC₅₀	1.6 μM Compound: 3, TPT	Cytotoxicity against p53-deficient human HeLa cells after 48 hrs by SRB assay Cytotoxicity against p53-deficient human HeLa cells after 48 hrs by SRB assay	[PMID: 19715319]
HeLa	IC₅₀	376 nM Compound: Topotecan	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 24900725]
HeLa	CC₅₀	4.5 μM Compound: Tpc	Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 3 days by fluorometric assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 3 days by fluorometric assay	[PMID: 32786885]
Hep 3B2	GI₅₀	0.22 μM Compound: Topotecan	Growth inhibition of human Hep3B cells after 72 hrs by XTT assay Growth inhibition of human Hep3B cells after 72 hrs by XTT assay	[PMID: 22079254]
Hep 3B2	GI₅₀	0.22 μM Compound: Topotecan	Antiproliferative activity against human Hep3B cells after 72 hrs by XTT assay Antiproliferative activity against human Hep3B cells after 72 hrs by XTT assay	[PMID: 19796956]
Hep 3B2	GI₅₀	0.4 μM Compound: 3, TPT	Cytotoxicity against p53-deficient human Hep3B cells after 48 hrs by SRB assay Cytotoxicity against p53-deficient human Hep3B cells after 48 hrs by SRB assay	[PMID: 19715319]
Hep 3B2	IC₅₀	1.4 μM Compound: 3, TPT	Cytotoxicity against p53-deficient human Hep3B cells after 48 hrs by SRB assay Cytotoxicity against p53-deficient human Hep3B cells after 48 hrs by SRB assay	[PMID: 19715319]
Hep 3B2	IC₅₀	7.9 nM Compound: Topotecan	Cytotoxicity against human Hep3B cells assessed as growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human Hep3B cells assessed as growth inhibition measured after 72 hrs by MTT assay	[PMID: 31881457]
HepG2	IC₅₀	0.06 μM Compound: 2, TPT	Cytotoxicity against human HepG2 cells after 4 days by MTT assay Cytotoxicity against human HepG2 cells after 4 days by MTT assay	[PMID: 18554906]
HepG2	IC₅₀	0.237 μM Compound: Topotecan	Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 30227711]
HepG2	GI₅₀	1.2 μM Compound: 3, TPT	Cytotoxicity against human HepG2 cells expressing wild type p53 after 48 hrs by SRB assay Cytotoxicity against human HepG2 cells expressing wild type p53 after 48 hrs by SRB assay	[PMID: 19715319]
HepG2	IC₅₀	1.6 μM Compound: 3, TPT	Cytotoxicity against human HepG2 cells expressing wild type p53 after 48 hrs by SRB assay Cytotoxicity against human HepG2 cells expressing wild type p53 after 48 hrs by SRB assay	[PMID: 19715319]
HepG2	IC₅₀	1.66 μM Compound: TPT	Antiproliferative activity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 24826818]
HepG2	IC₅₀	2.55 μM Compound: TPT	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 26725027]
HepG2	IC₅₀	3.28 μM Compound: TPT	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 34990980]
HepG2	IC₅₀	3.3 μM Compound: Topotecan	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay	[PMID: 35238576]
HepG2	GI₅₀	3.83 μM Compound: Topotecan	Growth inhibition of human HepG2 cells after 72 hrs by XTT assay Growth inhibition of human HepG2 cells after 72 hrs by XTT assay	[PMID: 22079254]
HepG2	GI₅₀	3.83 μM Compound: Topotecan	Antiproliferative activity against human HepG2 cells after 72 hrs by XTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by XTT assay	[PMID: 19796956]
HGC-27	IC₅₀	0.22 μM Compound: TPT	Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 34990980]
HGC-27	IC₅₀	10.82 μM Compound: TPT	Antiproliferative activity against human HGC-27 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human HGC-27 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34774339]
HL-60	IC₅₀	0.012 μM Compound: 3	Antitumor activity against human HL60 cells by SRB method Antitumor activity against human HL60 cells by SRB method	[PMID: 19541483]
HL-60	IC₅₀	0.052 μM Compound: 2, TPT	Cytotoxicity against human HL60 cells after 3 days Cytotoxicity against human HL60 cells after 3 days	[PMID: 21333532]
HL-60	IC₅₀	1 μM Compound: 5al	Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cells Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cells	[PMID: 8410981]
HMLE	IC₅₀	0.75 μM Compound: TPT	Antiproliferative activity against human HMLE cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human HMLE cells assessed as reduction in cell viability by MTT assay	[PMID: 28197320]
HOP-62	GI₅₀	0.01 μM Compound: 2	Growth inhibition of human HOP62 cells by five-dose growth inhibition assay Growth inhibition of human HOP62 cells by five-dose growth inhibition assay	[PMID: 25909279]
HT-1080	IC₅₀	0.18 μM Compound: Topotecan	Antiproliferative activity against human HT1080 cells assessed as growth inhibition incubated for 48 hrs by sulforhodamine B assay Antiproliferative activity against human HT1080 cells assessed as growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 26408815]
HT-1080	IC₅₀	0.5 μM Compound: Tpt	Antiproliferative activity against human HT1080 cells after 48 hrs by SRB assay Antiproliferative activity against human HT1080 cells after 48 hrs by SRB assay	[PMID: 29936355]
HT-29	IC₅₀	> 1000 nM Compound: 7	Cytotoxicity against human HT-29 cells after 72 hrs by alamar blue assay Cytotoxicity against human HT-29 cells after 72 hrs by alamar blue assay	[PMID: 21341674]
HT-29	GI₅₀	0.08 μM Compound: 3, TPT	Cytotoxicity against human HT-29 cells expressing p53 mutant after 48 hrs by SRB assay Cytotoxicity against human HT-29 cells expressing p53 mutant after 48 hrs by SRB assay	[PMID: 19715319]
HT-29	IC₅₀	0.23 μM Compound: Topotecan	Antiproliferative activity against human HT-29 cells assessed as growth inhibition incubated for 48 hrs by sulforhodamine B assay Antiproliferative activity against human HT-29 cells assessed as growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 26408815]
HT-29	IC₅₀	0.375 μM Compound: Topotecan	Cytotoxicity against human HT-29 cells by SRB method Cytotoxicity against human HT-29 cells by SRB method	[PMID: 18986807]
HT-29	IC₅₀	0.4 μM Compound: 3, TPT	Cytotoxicity against human HT-29 cells expressing p53 mutant after 48 hrs by SRB assay Cytotoxicity against human HT-29 cells expressing p53 mutant after 48 hrs by SRB assay	[PMID: 19715319]
HT-29	IC₅₀	0.41 μM Compound: Tpt	Antiproliferative activity against human HT-29 cells after 48 hrs by SRB assay Antiproliferative activity against human HT-29 cells after 48 hrs by SRB assay	[PMID: 29936355]
HT-29	IC₅₀	0.41 μM Compound: 3	Antitumor activity against human HT-29 cells by SRB method Antitumor activity against human HT-29 cells by SRB method	[PMID: 19541483]
HT-29	IC₅₀	0.88 μM Compound: 2, TPT	Cytotoxicity against human HT29 cells after 4 days by MTT assay Cytotoxicity against human HT29 cells after 4 days by MTT assay	[PMID: 18554906]
HT-29	IC₅₀	1.35 μM Compound: topotecan	Antiproliferative activity against human HT29 cells after 1 hr of drug exposure measured after 72 hrs Antiproliferative activity against human HT29 cells after 1 hr of drug exposure measured after 72 hrs	[PMID: 18424133]
HT-29	IC₅₀	25 nM Compound: 3	Human tumor cell cytotoxicity assay was performed using MTT (HT-29 cell line ) Human tumor cell cytotoxicity assay was performed using MTT (HT-29 cell line )	[PMID: 8576914]
HT-29	IC₅₀	25 nM Compound: Topotecan	Cytotoxicity was determined in vitro in HT-29 cells(colon) of human tumor cell lines by using MTT assay Cytotoxicity was determined in vitro in HT-29 cells(colon) of human tumor cell lines by using MTT assay	[PMID: 7853331]
HT-29	IC₅₀	3.28 μM Compound: TPT	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 34990980]
HT-29	IC₅₀	46.29 μM Compound: topotecan	Antiproliferative activity against BCRP overexpressing mitoxantrone-resistant human HT29 cells after 1 hr of drug exposure measured after 72 hrs Antiproliferative activity against BCRP overexpressing mitoxantrone-resistant human HT29 cells after 1 hr of drug exposure measured after 72 hrs	[PMID: 18424133]
Huh-7	IC₅₀	8.61 μM Compound: Topotecan	Antiproliferative activity against human HuH7 cells after 3 days by XTT assay Antiproliferative activity against human HuH7 cells after 3 days by XTT assay	[PMID: 24727241]
Huh-7	IC₅₀	8.61 μM Compound: Topotecan	Antiproliferative activity against human HuH7 cells after 72 hrs by XTT assay Antiproliferative activity against human HuH7 cells after 72 hrs by XTT assay	[PMID: 26686931]
IGROV-1	IC₅₀	160 nM Compound: 7	Cytotoxicity against human IGROV1 cells after 72 hrs by alamar blue assay Cytotoxicity against human IGROV1 cells after 72 hrs by alamar blue assay	[PMID: 21341674]
K562	IC₅₀	0.91 μM Compound: Topotecan	Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay	[PMID: 35238576]
K562	IC₅₀	1.15 μM Compound: TPT	Antiproliferative activity against human K562 cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability by MTT assay	[PMID: 28197320]
K562	IC₅₀	1.7 μM Compound: 3, TPT	Cytotoxicity against p53-deficient human K562 cells after 48 hrs by SRB assay Cytotoxicity against p53-deficient human K562 cells after 48 hrs by SRB assay	[PMID: 19715319]
K562	IC₅₀	500 nM Compound: Topotecan	Cytotoxicity against human K562 cells after 72 hrs by MTT assay Cytotoxicity against human K562 cells after 72 hrs by MTT assay	[PMID: 24900725]
KB	IC₅₀	> 200 μM Compound: TPT	Antiproliferative activity against human KB cells assessed as growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human KB cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 24826818]
KB	IC₅₀	0.0625 μM Compound: 2	Cytotoxicity against human KB cells after 72 hrs sulforhodamine B colorimetric assay Cytotoxicity against human KB cells after 72 hrs sulforhodamine B colorimetric assay	[PMID: 25008456]
KB	IC₅₀	0.063 μM Compound: 2	Cytotoxicity against human KB cells after 72 hrs by SRB assay Cytotoxicity against human KB cells after 72 hrs by SRB assay	[PMID: 25438769]
KB	IC₅₀	0.07 μM Compound: Topotecan	Cytotoxicity against human KB cells after 3 days by MTT assay Cytotoxicity against human KB cells after 3 days by MTT assay	[PMID: 20392545]
KB	IC₅₀	0.101 μM Compound: 3; TPT	Cytotoxicity against human KB cells after 72 hrs by SRB assay Cytotoxicity against human KB cells after 72 hrs by SRB assay	[PMID: 28789891]
KB	IC₅₀	0.22 μM Compound: 2, TPT	Cytotoxicity against human KB cells after 4 days by MTT assay Cytotoxicity against human KB cells after 4 days by MTT assay	[PMID: 18554906]
KB	IC₅₀	102 nM Compound: 3	Cytotoxicity against human KB cells after 72 hrs by SRB assay Cytotoxicity against human KB cells after 72 hrs by SRB assay	[PMID: 28927790]
KB	IC₅₀	102 nM Compound: 3	Cytotoxicity against human KB cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human KB cells after 72 hrs by sulforhodamine B assay	[PMID: 28285912]
KB	IC₅₀	2.61 μM Compound: Topotecan	Cytotoxicity in human KB cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human KB cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 30227711]
KB	IC₅₀	71.8 nM Compound: Topotecan	Cytotoxicity against human KB cells assessed as growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human KB cells assessed as growth inhibition measured after 72 hrs by MTT assay	[PMID: 31881457]
KB 3-1	IC₅₀	0.04 μM Compound: Topotecan	Cytotoxicity against human KB3-1 cells after MTT assay Cytotoxicity against human KB3-1 cells after MTT assay	[PMID: 18829334]
KB 3-1	IC₅₀	0.04 μM Compound: TPT	Cytotoxicity against human KB3-1 cells after 4 days by MTT method Cytotoxicity against human KB3-1 cells after 4 days by MTT method	[PMID: 19303306]
KB 3-1	IC₅₀	0.04 μM Compound: Topotecan	Cytotoxicity against human KB3-1 cells by MTT method Cytotoxicity against human KB3-1 cells by MTT method	[PMID: 19012996]
KB 3-1	IC₅₀	0.04 μM Compound: topotecan	Cytotoxicity against human KB3-1 cells by MTT method Cytotoxicity against human KB3-1 cells by MTT method	[PMID: 18771930]
KB-V1	IC₅₀	0.44 μM Compound: Topotecan	Cytotoxicity against multidrug resistant human KBV-1 cells overexpressing MDR1 after MTT assay Cytotoxicity against multidrug resistant human KBV-1 cells overexpressing MDR1 after MTT assay	[PMID: 18829334]
KB-V1	IC₅₀	0.44 μM Compound: TPT	Cytotoxicity against MDR1 overexpressing human KBV1 cells after 4 days by MTT method Cytotoxicity against MDR1 overexpressing human KBV1 cells after 4 days by MTT method	[PMID: 19303306]
KB-V1	IC₅₀	0.44 μM Compound: Topotecan	Cytotoxicity against multidrug resistant human KBV1 cells overexpressing MDR1 by MTT method Cytotoxicity against multidrug resistant human KBV1 cells overexpressing MDR1 by MTT method	[PMID: 19012996]
KB-V1	IC₅₀	0.44 μM Compound: topotecan	Cytotoxicity against human KBV1 cells by MTT method Cytotoxicity against human KBV1 cells by MTT method	[PMID: 18771930]
KETR3	IC₅₀	0.0049 μM Compound: topotecan	Cytotoxicity against human Ketr3 cells after 96 hrs by MTT assay Cytotoxicity against human Ketr3 cells after 96 hrs by MTT assay	[PMID: 15165144]
LNCaP	IC₅₀	9 nM Compound: 7	Cytotoxicity against human LNCAP cells after 72 hrs by alamar blue assay Cytotoxicity against human LNCAP cells after 72 hrs by alamar blue assay	[PMID: 21341674]
LoVo	IC₅₀	0.02 μM Compound: 2, Hycamtin	Cytotoxicity against human LoVo cells after 72 hrs by MTT assay Cytotoxicity against human LoVo cells after 72 hrs by MTT assay	[PMID: 20371183]
LoVo	IC₅₀	0.036 μM Compound: topotecan, TPT	Antitumor activity against human LOVO cells after 4 hrs by MTT assay Antitumor activity against human LOVO cells after 4 hrs by MTT assay	[PMID: 18207748]
LoVo	IC₅₀	1.21 μM Compound: Topotecan	Cytotoxicity against human LoVo cells after 3 days by MTT assay Cytotoxicity against human LoVo cells after 3 days by MTT assay	[PMID: 20202723]
LoVo	IC₅₀	11.6 nM Compound: Topotecan	Cytotoxic potentiation of Topotecan (TP) by the compound in (human colorectal cancer LoVo cell line Cytotoxic potentiation of Topotecan (TP) by the compound in (human colorectal cancer LoVo cell line	[PMID: 12408707]
LOX IMVI	IC₅₀	5 nM Compound: Topotecan	Cytotoxicity was determined in vitro in LOX cells (melanoma) of human tumor cell lines by using MTT assay Cytotoxicity was determined in vitro in LOX cells (melanoma) of human tumor cell lines by using MTT assay	[PMID: 7853331]
M21	IC₅₀	1.4 μM Compound: Tpt	Antiproliferative activity against human M21 cells after 48 hrs by SRB assay Antiproliferative activity against human M21 cells after 48 hrs by SRB assay	[PMID: 29936355]
M21	IC₅₀	1.4 μM Compound: Topotecan	Antiproliferative activity against human M21 cells assessed as growth inhibition incubated for 48 hrs by sulforhodamine B assay Antiproliferative activity against human M21 cells assessed as growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 26408815]
Malme-3M	IC₅₀	1000 nM Compound: 7	Cytotoxicity against human MALME-3M cells after 72 hrs by alamar blue assay Cytotoxicity against human MALME-3M cells after 72 hrs by alamar blue assay	[PMID: 21341674]
MCF7	GI₅₀	> 10 μM Compound: Topotecan	Growth inhibition of human MCF7 cells after 72 hrs by XTT assay Growth inhibition of human MCF7 cells after 72 hrs by XTT assay	[PMID: 22079254]
MCF7	IC₅₀	0.0018 μM Compound: topotecan	Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay	[PMID: 15165144]
MCF7	GI₅₀	0.01 μM Compound: 2	Growth inhibition of human MCF7 cells by five-dose growth inhibition assay Growth inhibition of human MCF7 cells by five-dose growth inhibition assay	[PMID: 25909279]
MCF7	IC₅₀	0.024 μM Compound: Topotecan	Antiproliferative activity against human MCF7 cells assessed as growth inhibition incubated for 48 hrs by sulforhodamine B assay Antiproliferative activity against human MCF7 cells assessed as growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 26408815]
MCF7	GI₅₀	0.04 μM Compound: topotecan	Growth inhibition of adriamycin-resistant MCF7 cells after 4 days Growth inhibition of adriamycin-resistant MCF7 cells after 4 days	[PMID: 17418582]
MCF7	GI₅₀	0.05 μM Compound: topotecan	Growth inhibition of MCF7 cells after 4 days Growth inhibition of MCF7 cells after 4 days	[PMID: 17418582]
MCF7	IC₅₀	0.14 μM Compound: Topotecan	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay	[PMID: 35238576]
MCF7	IC₅₀	0.15 μM Compound: Topotecan	Cytotoxicity against human MCF7 cells after 3 days by MTT assay Cytotoxicity against human MCF7 cells after 3 days by MTT assay	[PMID: 20392545]
MCF7	IC₅₀	0.2 μM Compound: Tpt	Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay	[PMID: 29936355]
MCF7	IC₅₀	0.26 μM Compound: TPT	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 34990980]
MCF7	IC₅₀	0.28 μM Compound: 3; TPT	Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay	[PMID: 28789891]
MCF7	GI₅₀	0.35 μM Compound: TPT	Cytotoxicity against human MCF-7 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MCF-7 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 34008967]
MCF7	IC₅₀	0.48 μM Compound: Topotecan	Inhibition of DNA topoisomerase 2 in human MCF7 cells incubated for 18 to 24 hrs by kinase assay Inhibition of DNA topoisomerase 2 in human MCF7 cells incubated for 18 to 24 hrs by kinase assay	[PMID: 31416740]
MCF7	IC₅₀	0.488 μM Compound: topotecan, TPT	Antitumor activity against human MCF7 cells after 4 hrs by MTT assay Antitumor activity against human MCF7 cells after 4 hrs by MTT assay	[PMID: 18207748]
MCF7	GI₅₀	0.8 μM Compound: 3, TPT	Cytotoxicity against estrogen receptor-positive human MCF7 cells expressing wild type p53 after 48 hrs by SRB assay Cytotoxicity against estrogen receptor-positive human MCF7 cells expressing wild type p53 after 48 hrs by SRB assay	[PMID: 19715319]
MCF7	IC₅₀	1.2 μM Compound: 2, TPT	Cytotoxicity against human MCF7 cells after 4 days by MTT assay Cytotoxicity against human MCF7 cells after 4 days by MTT assay	[PMID: 18554906]
MCF7	IC₅₀	1.8 μM Compound: Topotecan	Poison activity at TOP1 in human MCF7 cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA mobility measured after 30 mins by ethidium bromide staining based agarose gel electrophoresis Poison activity at TOP1 in human MCF7 cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA mobility measured after 30 mins by ethidium bromide staining based agarose gel electrophoresis	[PMID: 30897325]
MCF7	IC₅₀	1.9 μM Compound: Topotecan	Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay	[PMID: 16792409]
MCF7	IC₅₀	14.3 μM Compound: TPT	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 24826818]
MCF7	IC₅₀	2 μM Compound: 3, TPT	Cytotoxicity against estrogen receptor-positive human MCF7 cells expressing wild type p53 after 48 hrs by SRB assay Cytotoxicity against estrogen receptor-positive human MCF7 cells expressing wild type p53 after 48 hrs by SRB assay	[PMID: 19715319]
MCF7	IC₅₀	2.135 μM Compound: Topotecan	Cytotoxicity in human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 30227711]
MCF7	GI₅₀	2.59 μM Compound: TPT	Cytotoxicity against human MCF-7/TDP1 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MCF-7/TDP1 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 34008967]
MCF7	IC₅₀	3.46 μM Compound: Topotecan	Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay	[PMID: 25147141]
MCF7	IC₅₀	34.5 nM Compound: Topotecan	Cytotoxicity against human MCF7 cells assessed as growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as growth inhibition measured after 72 hrs by MTT assay	[PMID: 31881457]
MCF7	IC₅₀	5.55 μM Compound: 2, TPT	Cytotoxicity against human MCF7 cells by MTT assay Cytotoxicity against human MCF7 cells by MTT assay	[PMID: 19056266]
MCF7	IC₅₀	5.97 μM Compound: Topotecan	Antiproliferative activity against human MCF7 cells after 3 days by XTT assay Antiproliferative activity against human MCF7 cells after 3 days by XTT assay	[PMID: 24727241]
MCF7	IC₅₀	5.97 μM Compound: Top	Antiproliferative activity against human MCF7 cells after 72 hrs by XTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by XTT assay	[PMID: 23237975]
MCF7	IC₅₀	63 nM Compound: Topotecan	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 24900725]
MCF7	IC₅₀	666 nM Compound: 3	Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay	[PMID: 28927790]
MCF7	IC₅₀	666 nM Compound: 3	Cytotoxicity against human MCF7 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human MCF7 cells after 72 hrs by sulforhodamine B assay	[PMID: 28285912]
MDA-MB-231	IC₅₀	< 0.1 μM Compound: Topotecan	Antiproliferative activity against human MDA-MB-231 cells after 3 days by XTT assay Antiproliferative activity against human MDA-MB-231 cells after 3 days by XTT assay	[PMID: 24727241]
MDA-MB-231	IC₅₀	< 0.1 μM Compound: Topotecan	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by XTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by XTT assay	[PMID: 26686931]
MDA-MB-231	IC₅₀	< 0.1 μM Compound: Top	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by XTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by XTT assay	[PMID: 23237975]
MDA-MB-231	IC₅₀	> 500 nM Compound: Topotecan	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 24900725]
MDA-MB-231	GI₅₀	0.078 μM Compound: Topotecan	Growth inhibition of human MDA-MB-231 cells after 72 hrs by XTT assay Growth inhibition of human MDA-MB-231 cells after 72 hrs by XTT assay	[PMID: 22079254]
MDA-MB-231	IC₅₀	0.1 μM Compound: 2	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay	[PMID: 25438769]
MDA-MB-231	IC₅₀	0.102 μM Compound: 2	Cytotoxicity against human MDA-MB-231 cells after 72 hrs sulforhodamine B colorimetric assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs sulforhodamine B colorimetric assay	[PMID: 25008456]
MDA-MB-231	IC₅₀	0.77 μM Compound: 3; TPT	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay	[PMID: 28789891]
MDA-MB-231	IC₅₀	1.898 μM Compound: Topotecan	Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 30227711]
MDA-MB-231	IC₅₀	101.5 nM Compound: Topotecan	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by MTT assay	[PMID: 31881457]
MDA-MB-231	IC₅₀	773 nM Compound: 3	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay	[PMID: 28927790]
MDA-MB-231	IC₅₀	773 nM Compound: 3	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay	[PMID: 28285912]
MDA-MB-435	IC₅₀	< 0.001 μM Compound: 2, Hycamtin	Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay	[PMID: 20371183]
MDA-MB-435	GI₅₀	0.034 μM Compound: TPT	Cytotoxicity against human MDA-MB-435 cells incubated for 72 hrs by MTT assay Cytotoxicity against human MDA-MB-435 cells incubated for 72 hrs by MTT assay	[PMID: 22867019]
MDA-MB-435	IC₅₀	0.079 μM Compound: Topotecan	Cytotoxicity against human MDA-MB-435 cells after 3 days by MTT assay Cytotoxicity against human MDA-MB-435 cells after 3 days by MTT assay	[PMID: 20202723]
MDA-MB-435	IC₅₀	0.4 μM Compound: TPT	Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay	[PMID: 26226379]
MDA-MB-435	IC₅₀	0.448 μM Compound: TPT, Hycamptin	Cytotoxicity against human MDA-MB-435 cells after 3 days by MTT assay Cytotoxicity against human MDA-MB-435 cells after 3 days by MTT assay	[PMID: 21463912]
MDA-MB-435	IC₅₀	0.917 μM Compound: TPT	Antiproliferative activity against human MDA-MB-435 cells after 3 days by MTT assay Antiproliferative activity against human MDA-MB-435 cells after 3 days by MTT assay	[PMID: 23084702]
MES-SA	IC₅₀	4 nM Compound: 7	Cytotoxicity against human MESSA cells after 72 hrs by alamar blue assay Cytotoxicity against human MESSA cells after 72 hrs by alamar blue assay	[PMID: 21341674]
MES-SA/Dx5	IC₅₀	33 nM Compound: 7	Cytotoxicity against human MES-SA/Dx5 cells overexpressing MDR1 after 72 hrs by alamar blue assay Cytotoxicity against human MES-SA/Dx5 cells overexpressing MDR1 after 72 hrs by alamar blue assay	[PMID: 21341674]
MGC-803	IC₅₀	0.19 μM Compound: Topotecan	Cytotoxicity in human MGC803 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human MGC803 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 30227711]
MGC-803	IC₅₀	0.74 μM Compound: TPT	Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34774339]
MOLT-4	IC₅₀	19 nM Compound: Topotecan	Cytotoxicity against human MOLT4 cells after 72 hrs by MTT assay Cytotoxicity against human MOLT4 cells after 72 hrs by MTT assay	[PMID: 24900725]
MRC5	IC₅₀	4.25 μM Compound: Topotecan	Antiproliferative activity against human MRC5 cells after 72 hrs by XTT assay Antiproliferative activity against human MRC5 cells after 72 hrs by XTT assay	[PMID: 26686931]
MRC5	GI₅₀	4.25 μM Compound: Topotecan	Cytotoxicity against human MRC5 cells after 72 hrs by XTT assay Cytotoxicity against human MRC5 cells after 72 hrs by XTT assay	[PMID: 19796956]
NCI-H1299	GI₅₀	> 10 μM Compound: Topotecan	Growth inhibition of human H1299 cells after 72 hrs by XTT assay Growth inhibition of human H1299 cells after 72 hrs by XTT assay	[PMID: 22079254]
NCI-H1299	GI₅₀	> 10 μM Compound: Topotecan	Antiproliferative activity against human H1299 cells after 72 hrs by XTT assay Antiproliferative activity against human H1299 cells after 72 hrs by XTT assay	[PMID: 19796956]
NCI-H1299	IC₅₀	10.97 μM Compound: TPT	Antiproliferative activity against human NCI-H1299 cells assessed as growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 24826818]
NCI-H1299	IC₅₀	4.18 μM Compound: Topotecan	Antiproliferative activity against human H1299 cells after 24 hrs by MTT assay Antiproliferative activity against human H1299 cells after 24 hrs by MTT assay	[PMID: 25147141]
NCI-H1299	IC₅₀	6.02 μM Compound: Topotecan	Antiproliferative activity against human H1299 cells after 3 days by XTT assay Antiproliferative activity against human H1299 cells after 3 days by XTT assay	[PMID: 24727241]
NCI-H1299	IC₅₀	6.02 μM Compound: Topotecan	Antiproliferative activity against human H1299 cells after 72 hrs by XTT assay Antiproliferative activity against human H1299 cells after 72 hrs by XTT assay	[PMID: 26686931]
NCI-H1299	IC₅₀	6.02 μM Compound: Top	Antiproliferative activity against human H1299 cells after 72 hrs by XTT assay Antiproliferative activity against human H1299 cells after 72 hrs by XTT assay	[PMID: 23237975]
NCI-H460	GI₅₀	> 1000 nM Compound: 20	Cytotoxicity against human mitoxantrone-resistant H460 cells after 72 hrs by MTT assay Cytotoxicity against human mitoxantrone-resistant H460 cells after 72 hrs by MTT assay	[PMID: 24502276]
NCI-H460	IC₅₀	0.008 μg/mL Compound: topotecan	Antiproliferative activity against human NCI-H460 cells after 72 hrs Antiproliferative activity against human NCI-H460 cells after 72 hrs	[PMID: 17190463]
NCI-H460	IC₅₀	0.016 μM Compound: Topotecan	Antiproliferative activity against human NCI-H460 cells after 72 hrs by coulter counter analysis Antiproliferative activity against human NCI-H460 cells after 72 hrs by coulter counter analysis	[PMID: 21783369]
NCI-H460	IC₅₀	0.036 μM Compound: 3	Antitumor activity against human NCI-H460 cells by SRB method Antitumor activity against human NCI-H460 cells by SRB method	[PMID: 19541483]
NCI-H460	IC₅₀	1.18 μM Compound: topotecan	Cytotoxicity against human NCI-H460 cells after 1 hr Cytotoxicity against human NCI-H460 cells after 1 hr	[PMID: 18248813]
NCI-H460	IC₅₀	1.18 μM Compound: topotecan	Antiproliferative activity against human H460 cells after 1 hr of drug exposure measured after 72 hrs Antiproliferative activity against human H460 cells after 1 hr of drug exposure measured after 72 hrs	[PMID: 18424133]
NCI-H460	IC₅₀	1.38 μM Compound: Topotecan	In vitro cytotoxicity against H460 a human non-small lung carcinoma cell line after 1 hour drug exposure In vitro cytotoxicity against H460 a human non-small lung carcinoma cell line after 1 hour drug exposure	[PMID: 11212094]
NCI-H460	IC₅₀	1.75 μM Compound: Topotecan	Antiproliferative activity against human NCI-H460 cells after 1 hr by coulter counter analysis Antiproliferative activity against human NCI-H460 cells after 1 hr by coulter counter analysis	[PMID: 21783369]
NCI-H460	IC₅₀	110 nM Compound: 7	Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay in presence of 40 mg/ml HSA Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay in presence of 40 mg/ml HSA	[PMID: 21341674]
NCI-H460	GI₅₀	44.67 nM Compound: 20	Cytotoxicity against human H460 cells after 72 hrs by MTT assay Cytotoxicity against human H460 cells after 72 hrs by MTT assay	[PMID: 24502276]
NCI-H460	IC₅₀	45 nM Compound: 7	Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay	[PMID: 21341674]
NCI-H460	IC₅₀	7.1 μM Compound: Topotecan	Concentration causing 50% decrease of topotecan-resistant subline (H460/TPT) cell growth over that of untreated control. Concentration causing 50% decrease of topotecan-resistant subline (H460/TPT) cell growth over that of untreated control.	[PMID: 11052801]
NCI-H460	IC₅₀	7.29 μM Compound: Top	Antiproliferative activity against human H460 cells after 72 hrs by XTT assay Antiproliferative activity against human H460 cells after 72 hrs by XTT assay	[PMID: 23237975]
NCI-H69	IC₅₀	15.9 nM Compound: Topotecan	Cytotoxicity measured using the H69 parental (H69/P) human small cell lung carcinoma cell line Cytotoxicity measured using the H69 parental (H69/P) human small cell lung carcinoma cell line	[PMID: 11806724]
NCI-H69	IC₅₀	6 nM Compound: 7	Cytotoxicity against human H69 cells after 72 hrs by alamar blue assay Cytotoxicity against human H69 cells after 72 hrs by alamar blue assay	[PMID: 21341674]
NCI-H69	IC₅₀	62.9 nM Compound: Topotecan	Cytotoxicity measured using the drug resistant, P-glycoprotein (Pgp) expressing human small cell lung carcinoma cell line H69/LX4 Cytotoxicity measured using the drug resistant, P-glycoprotein (Pgp) expressing human small cell lung carcinoma cell line H69/LX4	[PMID: 11806724]
OVCAR-3	GI₅₀	0.22 μM Compound: 2	Growth inhibition of human OVCAR3 cells by five-dose growth inhibition assay Growth inhibition of human OVCAR3 cells by five-dose growth inhibition assay	[PMID: 25909279]
P388	IC₅₀	> 10 μM Compound: topotecan	Cytotoxicity against camptothecin-resistant mouse P388 cells by MTT method Cytotoxicity against camptothecin-resistant mouse P388 cells by MTT method	[PMID: 18771930]
P388	IC₅₀	0.045 μM Compound: Topotecan	Cytotoxicity against mouse P388 cells after MTT assay Cytotoxicity against mouse P388 cells after MTT assay	[PMID: 18829334]
P388	IC₅₀	0.045 μM Compound: Topotecan	Cytotoxicity against mouse P388 cells by MTT method Cytotoxicity against mouse P388 cells by MTT method	[PMID: 19012996]
P388	IC₅₀	0.045 μM Compound: topotecan	Cytotoxicity against mouse P388 cells by MTT method Cytotoxicity against mouse P388 cells by MTT method	[PMID: 18771930]
P388CPT45	IC₅₀	> 10 μM Compound: Topotecan	Cytotoxicity against camptothecin-resistant and TOP1 deficient mouse P388/CPT45 cells after MTT assay Cytotoxicity against camptothecin-resistant and TOP1 deficient mouse P388/CPT45 cells after MTT assay	[PMID: 18829334]
PC-3	IC₅₀	0.185 μM Compound: 4	Cytotoxicity against human PC3 cells expressing alpha5beta3 integrin assessed as cell survival after 72 hrs by SRB assay Cytotoxicity against human PC3 cells expressing alpha5beta3 integrin assessed as cell survival after 72 hrs by SRB assay	[PMID: 22959246]
PC-3	IC₅₀	1 μM Compound: Topotecan	Antiproliferative activity against human PC3 cells by [3H]thymidine incorporation assay Antiproliferative activity against human PC3 cells by [3H]thymidine incorporation assay	[PMID: 20932758]
PC-3	GI₅₀	1.3 μM Compound: 3, TPT	Cytotoxicity against p53-deficient human PC3 cells after 48 hrs by SRB assay Cytotoxicity against p53-deficient human PC3 cells after 48 hrs by SRB assay	[PMID: 19715319]
PC-3	IC₅₀	2 μM Compound: 3, TPT	Cytotoxicity against p53-deficient human PC3 cells after 48 hrs by SRB assay Cytotoxicity against p53-deficient human PC3 cells after 48 hrs by SRB assay	[PMID: 19715319]
PC-3	IC₅₀	3.99 μM Compound: 2, TPT	Cytotoxicity against human PC3 cells by MTT assay Cytotoxicity against human PC3 cells by MTT assay	[PMID: 19056266]
PC-3	IC₅₀	45 nM Compound: 7	Cytotoxicity against human PC3 cells after 72 hrs by alamar blue assay Cytotoxicity against human PC3 cells after 72 hrs by alamar blue assay	[PMID: 21341674]
PC-3	IC₅₀	62 nM Compound: Topotecan	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 24900725]
PC-3	IC₅₀	9.35 μM Compound: Topotecan	Antiproliferative activity against human PC3 cells after 72 hrs by XTT assay Antiproliferative activity against human PC3 cells after 72 hrs by XTT assay	[PMID: 26686931]
QGY-7703	IC₅₀	11.864 μM Compound: Topotecan	Cytotoxicity in human QGY7703 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human QGY7703 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 30227711]
RPMI 8402	IC₅₀	> 10 μM Compound: Topotecan	Cytotoxicity using camptothecin-resistant variant of RPM18402 (CPT-K5) possessing functional, but mutant TOP-1 Cytotoxicity using camptothecin-resistant variant of RPM18402 (CPT-K5) possessing functional, but mutant TOP-1	[PMID: 12392745]
RPMI 8402	IC₅₀	0.012 μM Compound: Topotecan	Cytotoxic activity against human lymphoblast tumor cell line RPMI8402 after 4 days of treatment Cytotoxic activity against human lymphoblast tumor cell line RPMI8402 after 4 days of treatment	[PMID: 12747798]
RPMI 8402	IC₅₀	0.021 μM Compound: Topotecan	Cytotoxicity against human RPMI8402 cells after MTT assay Cytotoxicity against human RPMI8402 cells after MTT assay	[PMID: 18829334]
RPMI 8402	IC₅₀	0.21 μM Compound: topotecan	Cytotoxicity against human RPMI8402 cells by MTT method Cytotoxicity against human RPMI8402 cells by MTT method	[PMID: 18771930]
RPMI-8226	IC₅₀	0.021 μM Compound: Topotecan	Cytotoxicity against human RPMI8226 cells by MTT method Cytotoxicity against human RPMI8226 cells by MTT method	[PMID: 19012996]
SF-539	GI₅₀	0.01 μM Compound: 2	Growth inhibition of human SF539 cells by five-dose growth inhibition assay Growth inhibition of human SF539 cells by five-dose growth inhibition assay	[PMID: 25909279]
Sf9	IC₅₀	0.021 μM Compound: Topotecan	Poison activity at recombinant human TOP1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA mobility measured after 30 mins by ethidium bromide staining based agarose gel electrophoresis Poison activity at recombinant human TOP1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA mobility measured after 30 mins by ethidium bromide staining based agarose gel electrophoresis	[PMID: 30897325]
SGC-7901	IC₅₀	> 10 μM Compound: Topotecan	Cytotoxicity in human SGC7901 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human SGC7901 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 30227711]
SGC-7901	IC₅₀	4.17 μM Compound: TPT	Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34774339]
SK-BR-3	IC₅₀	8.91 μM Compound: Top	Antiproliferative activity against human SKBR3 cells after 72 hrs by XTT assay Antiproliferative activity against human SKBR3 cells after 72 hrs by XTT assay	[PMID: 23237975]
SK-MEL-2	IC₅₀	140 nM Compound: 7	Cytotoxicity against human SK-MEL-2 cells after 72 hrs by alamar blue assay Cytotoxicity against human SK-MEL-2 cells after 72 hrs by alamar blue assay	[PMID: 21341674]
SK-N-SH	IC₅₀	0.093 μM Compound: Topotecan	Cytotoxicity in human SK-N-SH cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human SK-N-SH cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 30227711]
SK-OV-3	IC₅₀	44 nM Compound: 3	Human tumor cell cytotoxicity assay was performed using MTT (SK-OV3 cell line ) Human tumor cell cytotoxicity assay was performed using MTT (SK-OV3 cell line )	[PMID: 8576914]
SK-OV-3	IC₅₀	44 nM Compound: Topotecan	Cytotoxicity was determined in vitro in SK-OV-3 cells (ovarian) of human tumor cell lines by using MTT assay Cytotoxicity was determined in vitro in SK-OV-3 cells (ovarian) of human tumor cell lines by using MTT assay	[PMID: 7853331]
SK-VLB	IC₅₀	149 nM Compound: Topotecan	Cytotoxicity was determined in vitro in SKVLB cells(ovarian with upregulated MDRp-glycoprotein) of human tumor cell lines by using MTT assay Cytotoxicity was determined in vitro in SKVLB cells(ovarian with upregulated MDRp-glycoprotein) of human tumor cell lines by using MTT assay	[PMID: 7853331]
SK-VLB	IC₅₀	150 nM Compound: 3	Human tumor cell cytotoxicity assay was performed using MTT (SKVLB cell line ) Human tumor cell cytotoxicity assay was performed using MTT (SKVLB cell line )	[PMID: 8576914]
SMMC-7721	IC₅₀	11.627 μM Compound: Topotecan	Cytotoxicity in human SMMC7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human SMMC7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 30227711]
SN12C	GI₅₀	0.02 μM Compound: 2	Growth inhibition of human SN12C cells by five-dose growth inhibition assay Growth inhibition of human SN12C cells by five-dose growth inhibition assay	[PMID: 25909279]
SW-620	IC₅₀	> 500 nM Compound: 2	Antiproliferative activity against human SW-620 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human SW-620 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35932565]
SW-620	IC₅₀	3.2 nM Compound: Topotecan	Cytotoxic potentiation of Topotecan (TP) by the compound in human colon carcinoma SW620 cell line Cytotoxic potentiation of Topotecan (TP) by the compound in human colon carcinoma SW620 cell line	[PMID: 12408707]
T47D	IC₅₀	104 nM Compound: Topotecan	Cytotoxicity was determined in vitro in T47D cells(breast) of human tumor cell lines by using MTT assay Cytotoxicity was determined in vitro in T47D cells(breast) of human tumor cell lines by using MTT assay	[PMID: 7853331]
THP-1	IC₅₀	1.5 μM Compound: 3, TPT	Cytotoxicity against human THP1 cells expressing p53 mutant after 48 hrs by SRB assay Cytotoxicity against human THP1 cells expressing p53 mutant after 48 hrs by SRB assay	[PMID: 19715319]
U-251	EC₅₀	> 20 μM Compound: 6, TPT	Effect on basal transcription in human U251 cells co-transfected with pGL3 incubated for 24 hrs by luciferase reporter gene assay Effect on basal transcription in human U251 cells co-transfected with pGL3 incubated for 24 hrs by luciferase reporter gene assay	10.1039/C4MD00111G
U-251	IC₅₀	> 3 μM Compound: Topotecan	Inhibition of HIF1alpha in human U251 cells under normoxic condition by luciferase reporter gene assay Inhibition of HIF1alpha in human U251 cells under normoxic condition by luciferase reporter gene assay	[PMID: 20932758]
U-251	EC₅₀	0.012 μM Compound: 6, TPT	Inhibition of human HIF1alpha-mediated transcription expressed in human U251 cells co-transfected with pGL2-TK-HRE incubated for 24 hrs by luciferase reporter gene assay Inhibition of human HIF1alpha-mediated transcription expressed in human U251 cells co-transfected with pGL2-TK-HRE incubated for 24 hrs by luciferase reporter gene assay	10.1039/C4MD00111G
U-251	IC₅₀	0.06 μM Compound: Topotecan	Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay	[PMID: 20932758]
U-251	IC₅₀	0.37 μM Compound: Topotecan	Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 34537445]
U-251	IC₅₀	0.5 μM Compound: Topotecan	Antiproliferative activity against human U251 cells by [3H]thymidine incorporation assay Antiproliferative activity against human U251 cells by [3H]thymidine incorporation assay	[PMID: 20932758]
U-251	EC₅₀	54 nM Compound: 4b, NSC-609699, hycamtin	Inhibition of topoisomerase-1 in human U251 cells assessed as inhibition of hypoxia-induced HIF-1alpha accumulation in nuclear extract after 6 to 24 hrs by immunoblot analysis Inhibition of topoisomerase-1 in human U251 cells assessed as inhibition of hypoxia-induced HIF-1alpha accumulation in nuclear extract after 6 to 24 hrs by immunoblot analysis	[PMID: 22305612]
U-251	EC₅₀	71.3 nM Compound: 4b, NSC-609699, hycamtin	Inhibition of topoisomerase-1 in human U251 cells assessed as inhibition of HIF-1-mediated hypoxia-induced VEGF expression after 24 hrs by luciferase reporter gene assay Inhibition of topoisomerase-1 in human U251 cells assessed as inhibition of HIF-1-mediated hypoxia-induced VEGF expression after 24 hrs by luciferase reporter gene assay	[PMID: 22305612]
U-87MG ATCC	IC₅₀	0.06 μM Compound: Topotecan	Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 34537445]
U-87MG ATCC	IC₅₀	0.16 μM Compound: TPT	Antiproliferative activity against human U87 cells assessed as growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human U87 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 24826818]
U-937	IC₅₀	1.1 μM Compound: 3, TPT	Cytotoxicity against human U937 cells expressing p53 mutant after 48 hrs by SRB assay Cytotoxicity against human U937 cells expressing p53 mutant after 48 hrs by SRB assay	[PMID: 19715319]
UACC-62	GI₅₀	0.01 μM Compound: 2	Growth inhibition of human UACC62 cells by five-dose growth inhibition assay Growth inhibition of human UACC62 cells by five-dose growth inhibition assay	[PMID: 25909279]
WISH	IC₅₀	1.3 μM Compound: Topotecan	Cytotoxicity against human WISH cells after 96 hrs by MTT assay Cytotoxicity against human WISH cells after 96 hrs by MTT assay	[PMID: 16792409]

In Vitro

Topotecan obviously inhibits proliferation of human glioma cells and glioma stem cells (GSCs) in a dose- and time-dependent manner^[1].
Topotecan (0-40 μM) obviously inhibits the cell viability compared with the control groups, in a dose-dependent manner^[1].
Topotecan shows anti-proliferation activity against U251, U87, GSCs-U251 and GSCs-U87 cells, with IC₅₀ values of 2.73±0.25, 2.95±0.23, 5.46±0.41, and 5.95±0.24 μM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

NUB-7 metastatic model, the animals belonging to all the 4 groups are sacrificed after 14 days treatment. Compared with the control, Low dose metronomic (LDM) Topotecan (TP) and TP+Pazopanib (PZ) liver weights are significantly lower in TP+PZ-treated animals, compared with PZ. Microscopic tumors are visible in the livers of mice belonging to all the groups except TP+PZ confirming the ability of TP+PZ to control liver metastasis^[2].
Topotecan (0.5, 1.0, and 1.5 mg/kg; Orally, daily) causes greater reduction in microvascular density in an ovarian cancer model, but the mice treated with 1.5 mg/kg daily, oral Topotecan show decreased food intake, and a lesser antitumor effect^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

421.45

Formula

C₂₃H₂₃N₃O₅

CAS No.

123948-87-8

SMILES

O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=CC5=C(CN(C)C)C(O)=CC=C5N=C4C3=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (237.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3728 mL	11.8638 mL	23.7276 mL
5 mM	0.4746 mL	2.3728 mL	4.7455 mL
10 mM	0.2373 mL	1.1864 mL	2.3728 mL

View the Complete Stock Solution Preparation Table

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.93 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.93 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Zhang FL, et al. PLoS One. 2013 Nov 26;8(11):e81815.Topoisomerase I inhibitors, Shikonin and Topotecan, inhibit growth and induce apoptosis of glioma cells andglioma stem cells. [Content Brief]

[2]. Kumar S, et al. Metronomic oral topotecan with pazopanib is an active antiangiogenic regimen in mouse models of aggressive pediatric solid tumor. Clin Cancer Res. 2011 Sep 1;17(17):5656-67. [Content Brief]

Cell Assay ^[1]	The U251, U87, GSCs-U251 and GSCs-U87 cells are seeded at a density of 2×10⁴ cells per well in 96-well plates separately, and incubated for 24 h. Cells are administered with Shikonin and Topotecan (0.02, 0.2, 2, 20, 40 μM). After the treatment, 10 μL of cell counting kit-8 (CCK-8) is added into each well for additional 1-hour incubation at 37°C. The optical density (OD) is read with a microplate reader at 450 nm^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] For subcutaneous xenograft studies, we used SK-N-BE, SH-SY5Y, KHOS, and RH30. 1×10⁶ cells are implanted subcutaneously into the inguinal fat pad of each of nonobese diabetic/severe combined immune deficient (NOD/SCID) mice. When tumors reached 0.5 cm in diameter, the animals are randomized into 4 groups and treated daily by oral gavage. The animals are grouped as: Control group, LDM Topotecan group or LDM TP (1 mg/kg Topotecan), Pazopanib group or PZ (150 mg/kg Pazopanib) and combination group or TP+PZ (1 mg/kg Topotecan+150 mg/kg Pazopanib). To compare pulse Topotecan with LDM TP in KHOS osteosarcoma model, PZ is replaced by weekly oral dose of pulse Topotecan (SKF104864) or Pulse TP (15 mg/kg Topotecan (SKF104864)). The criteria for endpoint are tumor sizes exceeding 2.0 cm in diameter or animals showing signs of morbidity. The tumor sizes are measured on a daily basis until the endpoint or sacrifice. The long (D) and short diameters (d) are measured with calipers. Tumor volume (cm³) is calculated as V=0.5×D×d². When the endpoint is reached or at the end of the treatment, the animals are sacrificed by cervical dislocation. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Zhang FL, et al. PLoS One. 2013 Nov 26;8(11):e81815.Topoisomerase I inhibitors, Shikonin and Topotecan, inhibit growth and induce apoptosis of glioma cells andglioma stem cells. [Content Brief] [2]. Kumar S, et al. Metronomic oral topotecan with pazopanib is an active antiangiogenic regimen in mouse models of aggressive pediatric solid tumor. Clin Cancer Res. 2011 Sep 1;17(17):5656-67. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3728 mL	11.8638 mL	23.7276 mL	59.3190 mL
	5 mM	0.4746 mL	2.3728 mL	4.7455 mL	11.8638 mL
	10 mM	0.2373 mL	1.1864 mL	2.3728 mL	5.9319 mL
	15 mM	0.1582 mL	0.7909 mL	1.5818 mL	3.9546 mL
	20 mM	0.1186 mL	0.5932 mL	1.1864 mL	2.9660 mL
	25 mM	0.0949 mL	0.4746 mL	0.9491 mL	2.3728 mL
	30 mM	0.0791 mL	0.3955 mL	0.7909 mL	1.9773 mL
	40 mM	0.0593 mL	0.2966 mL	0.5932 mL	1.4830 mL
	50 mM	0.0475 mL	0.2373 mL	0.4746 mL	1.1864 mL
	60 mM	0.0395 mL	0.1977 mL	0.3955 mL	0.9887 mL
	80 mM	0.0297 mL	0.1483 mL	0.2966 mL	0.7415 mL
	100 mM	0.0237 mL	0.1186 mL	0.2373 mL	0.5932 mL

Topotecan Related Classifications

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Topotecan123948-87-8SKF 104864A NSC 609669NSC609669NSC 609669NSC-609669TopoisomeraseAutophagyApoptosisU251U87GSCs-U251GSCs-U87orally activeInhibitorinhibitorinhibit

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Topotecan (Synonyms: SKF 104864A; NSC 609669)

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