Lapatinib (Synonyms: GW572016; GW2016)

Name: Lapatinib
Brand: MedChemExpress
SKU: HY-50898
Rating: 5.0 (76 reviews)

Cat. No.: HY-50898 Purity: 99.83%: FAQs
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Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC₅₀ values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.

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

Lapatinib Chemical Structure

CAS No. : 231277-92-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
50 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 86	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 172	In-stock	Estimated Time of Arrival: December 31
1 g	USD 198	In-stock	Estimated Time of Arrival: December 31
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Based on 76 publication(s) in Google Scholar

Other Forms of Lapatinib:

Lapatinib ditosylate In-stock
Lapatinib-d7 ditosylate Get quote
Lapatinib-d₄ Get quote
Lapatinib-d₇ dihydrochloride Get quote
Lapatinib-d₅ Get quote
Lapatinib-d₄-1 Get quote
Lapatinib ditosylate monohydrate Get quote
Lapatinib tosylate Get quote
Lapatinib (Standard) Get quote

68 Publications Citing Use of MCE Lapatinib

: Lapatinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 25;37(1):123. [Abstract]; MCF-7 cells are treated with or without 5 μg/mL cisplatin (DDP) for 48 h after preincubated with or without Lapatinib at the indicated concentrations for 6 h, respectively. Then the levels of ER-α36, total EGFR and P-EGFR, total HER-2 and P-HER-2, total ERK and P-ERK are evaluated using western blot.

: Lapatinib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Mar;17(3):603-613. [Abstract]; Immunoblot analysis of U-CH1 cells treated with the indicated doses of inhibitors (Afatinib, Erlotinib and Lapatinib) for 2 h (upper panel) or 48 h (lower panel). Protein cell extracts are resolved on SDS-PAGE gel and membranes probed with the indicated antibodies. IC₅₀s of the different inhibitors are reported.

: Lapatinib purchased from MedChemExpress. Usage Cited in: Cancer Chemother Pharmacol. 2018 Sep;82(3):383-394. [Abstract]; The expression level of EGFR and HER2 on normal esophageal epithelium cell and four esophageal squamous cancer cell lines analyzed by western blot.

: Lapatinib purchased from MedChemExpress. Usage Cited in: Nature. 2017 Aug 24;548(7668):471-475. [Abstract]; Western blot of SKBR3, BT474, MDA-MB-453, and MDA-MB-361 cells treated with DMSO, Lapatinib, or Abemaciclib for 48 h. Western blot of MDA-MB-453 cells pretreated with DMSO or Abemaciclib (500 nM) for 0, 1, or 7 days before exposure to Staurosporine (500 nM) for 4 h.

: Lapatinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Aug 24;8(62):104894-104912. [Abstract]; MDA-MB-231 cells are serum-starved overnight and pre-treated with 3 μM Lapatinib or DMSO for 3 hours. After that time, cells are lysed (0hr) or stimulated with EGF for 1, 8, 24, 48, and 72 hours. Western blots of p-EGFR (Tyr1173), EGFR, p-cJun (ser63), cJun, and vinculin are shown with band densitometries beneath.

: Lapatinib purchased from MedChemExpress. Usage Cited in: Oncogene. 2016 Jun 9;35(23):2961-70. [Abstract]; Western blot analysis of p-AKT(T308), p-AKT(S473) and p-ERK in transplanted NIC⁺PIK3CA^H1047R tumors treated as indicated. Transplants of NIC⁺PIK3CA^H1047R primary mammary tumors are first established in immunodeficient nude mice maintained on Doxycycline. Treatment starts when tumor transplants reach 500 mm³. DOX On, on Doxycycline; DOX Off, Doxycycline withdrawal. Lapatinib, 100mg/kg/day, p.o; GDC-0941, 120mg/kg/ day, p.o. Tumo

: Lapatinib purchased from MedChemExpress. Usage Cited in: Oncogene. 2016 Jun 9;35(23):2961-70. [Abstract]; The combined use of MEK162 with HER kinase inhibitor Lapatinib, almost completely abolishes MAPK signaling as evidenced by diminished phospho-Erk levels. Western blot analyses of ERK signaling in tumor transplants from mice treated as indicated. Three hours after their dose on day four of treatment, the mice are sacrificed for analysis. Vinculin is used as a loading control.

: Lapatinib purchased from MedChemExpress. Usage Cited in: Tumour Biol. 2016 Nov;37(11):14831-14839. [Abstract]; Western blot analysis of PI3K signaling in cell lysates treated with Lapatinib (1 μM) with or without BYL719.

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Biological Activity
Purity & Documentation
References
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Description

Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC₅₀ values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively^[1].

IC₅₀ & Target^[1]

EGFR

10.2 nM (IC₅₀, Cell Free Assay)

ErbB2

9.8 nM (IC₅₀, Cell Free Assay)

Cellular Effect

Cell Line	Type	Value	Description	References
3T3	EC₅₀	13 μM Compound: 1	Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 48 hrs by chlorophenol red-beta-D-galactopyranoside based assay Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 48 hrs by chlorophenol red-beta-D-galactopyranoside based assay	[PMID: 28337329]
A2780	IC₅₀	10.4 μM Compound: Lapatinib	Antiproliferative activity against human A2780 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 31655429]
A2780	IC₅₀	10.4 μM Compound: Lapatinib	Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay	[PMID: 29684708]
A-431	IC₅₀	> 10000 nM Compound: Lapatinib	Inhibition of IGF1R intracellular phosphorylation in human A431 cells by ELISA Inhibition of IGF1R intracellular phosphorylation in human A431 cells by ELISA	[PMID: 20346655]
A-431	IC₅₀	0.15 μM Compound: 3; GW-572016	Antiproliferative activity against human A431 cells expressing EGFR/HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human A431 cells expressing EGFR/HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 27769671]
A-431	IC₅₀	0.97 μM Compound: 5, GW-572016	Cytotoxicity against human A431 cells overexpressing EGFR by resazurin dye reduction assay Cytotoxicity against human A431 cells overexpressing EGFR by resazurin dye reduction assay	[PMID: 21080629]
A-431	IC₅₀	104 nM Compound: 1	Cytotoxicity against human A431 cells overexpressing HER-1 gene after 72 hrs by SRB assay Cytotoxicity against human A431 cells overexpressing HER-1 gene after 72 hrs by SRB assay	[PMID: 22372864]
A-431	IC₅₀	104 nM Compound: 3	Cytotoxicity against human A431 cells after 72 hrs by SRB assay Cytotoxicity against human A431 cells after 72 hrs by SRB assay	[PMID: 19888761]
A-431	IC₅₀	2.6 μM Compound: 3	Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay	[PMID: 22595177]
A-431	IC₅₀	2.62 μM Compound: Lapatinib	Cytotoxicity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay Cytotoxicity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay	[PMID: 22182581]
A-431	IC₅₀	2.66 μM Compound: Lapatinib	Antiproliferative activity against human A431 cells after 72 hrs by MTT assay Antiproliferative activity against human A431 cells after 72 hrs by MTT assay	[PMID: 30508379]
A-431	IC₅₀	3.59 μM Compound: Lapatinib	Antiproliferative activity against human A431 cells overexpressing EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human A431 cells overexpressing EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32139324]
A-431	IC₅₀	4.8 μM Compound: Lapatinib	Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay	[PMID: 31202990]
A-431	IC₅₀	4.8 μM Compound: Lapatinib	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 29421573]
A-431	IC₅₀	4.8 μM Compound: Lapatinib	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 28711703]
A-431	IC₅₀	4.8 μM Compound: Lapatinib	Antiproliferative activity against human A-431 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human A-431 cells assessed as cell growth inhibition by MTT assay	[PMID: 32739648]
A-431	IC₅₀	52 nM Compound: Lapatinib	Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA	[PMID: 20346655]
A-431	IC₅₀	643.1 nM Compound: Lapatinib	Cytotoxicity against human A431 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human A431 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
A549	IC₅₀	0.51 μM Compound: 3; GW-572016	Cytotoxicity against human A549 cells expressing EGFR and KRAS mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human A549 cells expressing EGFR and KRAS mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 27769671]
A549	IC₅₀	11 μM Compound: Tykerb(R)	Antiproliferative activity against human A549 cells overexpressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells overexpressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31125894]
A549	IC₅₀	11.3 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs under normoxia condition by SRB assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs under normoxia condition by SRB assay	[PMID: 32739648]
A549	IC₅₀	13.26 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs under hypoxia condition by SRB assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs under hypoxia condition by SRB assay	[PMID: 32739648]
A549	IC₅₀	14.9 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 31202990]
A549	IC₅₀	14.9 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells harboring wild type EGFR/K-ras mutant after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring wild type EGFR/K-ras mutant after 72 hrs by MTT assay	[PMID: 29421573]
A549	IC₅₀	14.9 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells harboring wild type EGFR/K-Ras mutant after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring wild type EGFR/K-Ras mutant after 72 hrs by MTT assay	[PMID: 28711703]
A549	IC₅₀	14.9 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition by MTT assay	[PMID: 32739648]
A549	IC₅₀	3.64 μM Compound: Lapatinib	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30508379]
A549	IC₅₀	6.74 μM Compound: Lapatinib	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: 27187856]
A549	IC₅₀	8.5 μM Compound: 5, GW-572016	Cytotoxicity against human A549 cells overexpressing HDAC by resazurin dye reduction assay Cytotoxicity against human A549 cells overexpressing HDAC by resazurin dye reduction assay	[PMID: 21080629]
AU565	IC₅₀	0.064 μM Compound: Lapatinib	Antiproliferative activity against human AU565 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay Antiproliferative activity against human AU565 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay	[PMID: 33314925]
B16-F10	IC₅₀	0.21 μM Compound: Lapatinib	Antiproliferative activity against mouse B16F10 cells after 12 hrs by MTT assay Antiproliferative activity against mouse B16F10 cells after 12 hrs by MTT assay	[PMID: 26652482]
Bel-7402	IC₅₀	3.7 μM Compound: Lapatinib	Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay	[PMID: 28092860]
BT-474	IC₅₀	0.025 μM Compound: lapatinib	Antiproliferative activity against human BT474 cells after 72 hrs by methylene blue staining-based method Antiproliferative activity against human BT474 cells after 72 hrs by methylene blue staining-based method	[PMID: 21887403]
BT-474	IC₅₀	0.031 μM Compound: Lapatinib	Cytotoxicity against human BT474 cells expressing Her2 assessed as reduction in cell viability after 72 hrs by cell titer-glo luminescence assay Cytotoxicity against human BT474 cells expressing Her2 assessed as reduction in cell viability after 72 hrs by cell titer-glo luminescence assay	[PMID: 27288180]
BT-474	IC₅₀	0.037 μM Compound: Lapatinib	Antiproliferative activity against human BT474 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human BT474 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32139324]
BT-474	IC₅₀	0.064 μM Compound: Lapatinib	Antiproliferative activity against human BT474 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay Antiproliferative activity against human BT474 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay	[PMID: 33314925]
BT-474	IC₅₀	0.08 μM Compound: 1, GW-572016	Inhibition of BT474 cell growth after 72 hrs Inhibition of BT474 cell growth after 72 hrs	[PMID: 16777410]
BT-474	IC₅₀	0.1 μM Compound: Lapatinib	Antiproliferative activity against human BT474 cells after 3 days by methylene blue staining Antiproliferative activity against human BT474 cells after 3 days by methylene blue staining	[PMID: 22101132]
BT-474	IC₅₀	0.1 μM Compound: 3; GW-572016	Cytotoxicity against human BT474 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human BT474 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 27769671]
BT-474	GI₅₀	0.2 μM Compound: Lapatinib	Cytotoxicity against human BT474 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay Cytotoxicity against human BT474 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	[PMID: 29089259]
BT-474	GI₅₀	0.93 μM Compound: Lapatinib	Cytotoxicity against human BT474 cells expressing HER2 after 72 hrs by Cell Titer Glo assay Cytotoxicity against human BT474 cells expressing HER2 after 72 hrs by Cell Titer Glo assay	[PMID: 26475520]
BT-474	IC₅₀	140 nM Compound: Lapatinib	Inhibition of ERBb2 phosphorylation in human BT474 cells by ELISA Inhibition of ERBb2 phosphorylation in human BT474 cells by ELISA	[PMID: 20817523]
BT-474	IC₅₀	63.9 nM Compound: Lapatinib	Cytotoxicity against human BT474 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human BT474 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
CAL-27	IC₅₀	< 32 nM Compound: 5, GW-572016	Inhibition of EGF-induced EGFR phosphorylation in human CAL27 cells overexpressing EGFR after 16 hrs by Western blot Inhibition of EGF-induced EGFR phosphorylation in human CAL27 cells overexpressing EGFR after 16 hrs by Western blot	[PMID: 21080629]
CAL-27	IC₅₀	0.007 μM Compound: 5, GW-572016	Cytotoxicity against human CAL27 cells overexpressing EGFR by resazurin dye reduction assay Cytotoxicity against human CAL27 cells overexpressing EGFR by resazurin dye reduction assay	[PMID: 21080629]
CAL-27	IC₅₀	0.53 μM Compound: 5, Tykerb	Cytotoxicity against human CAL27 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human CAL27 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
Calu-3	IC₅₀	0.1 μM Compound: Lapatinib	Antiproliferative activity against human Calu3 cells after 72 hrs by MTT assay Antiproliferative activity against human Calu3 cells after 72 hrs by MTT assay	[PMID: 28092860]
Calu-3	IC₅₀	0.216 μM Compound: Lapatinib	Antiproliferative activity against human Calu3 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human Calu3 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32139324]
Calu-3	IC₅₀	0.23 μM Compound: Lapatinib	Cytotoxicity against human Calu3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human Calu3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
CAMA-1	IC₅₀	> 10 μM Compound: Lapatinib, Tykerb	Antiproliferative activity against human progesterone receptor and HER2 deficient CAMA1 cells expressing estrogen receptor after 72 hrs by MTT assay Antiproliferative activity against human progesterone receptor and HER2 deficient CAMA1 cells expressing estrogen receptor after 72 hrs by MTT assay	[PMID: 23927972]
COLO 205	IC₅₀	4.6 μM Compound: Lapatinib	Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay	[PMID: 28092860]
CWR22R	IC₅₀	6.06 μM Compound: 5, Tykerb	Cytotoxicity against human 22Rv1 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human 22Rv1 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
DU-145	IC₅₀	2.99 μM Compound: 5, Tykerb	Cytotoxicity against human DU145 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human DU145 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
DU-145	GI₅₀	20 μM Compound: Lapatinib	Antiproliferative activity against human DU145 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human DU145 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
EOL1	GI₅₀	0.41 μM Compound: Lapatinib	Cytotoxicity against human EOL-1 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay Cytotoxicity against human EOL-1 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	[PMID: 29089259]
HCC1954	IC₅₀	5 μM Compound: Tykerb(R)	Antiproliferative activity against human HCC1954 cells overexpressing HER2 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC1954 cells overexpressing HER2 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31125894]
HCC827	IC₅₀	0.6 μM Compound: Lapatinib	Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay	[PMID: 31202990]
HCC827	IC₅₀	0.6 μM Compound: Lapatinib	Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 del mutant after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 del mutant after 72 hrs by MTT assay	[PMID: 29421573]
HCC827	GI₅₀	22.3 μM Compound: Lapatinib	Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	[PMID: 29089259]
HCT-116	IC₅₀	10.12 μM Compound: Lapatinib	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 29684708]
HCT-116	IC₅₀	12 nM Compound: Lapatinib	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 33545637]
HCT-116	IC₅₀	13.14 μM Compound: 5, Tykerb	Cytotoxicity against human HCT116 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human HCT116 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
HCT-116	GI₅₀	20 μM Compound: Lapatinib	Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
HCT-116	IC₅₀	42.36 μM Compound: 3	Antiproliferative activity against human HCT116 cells by MTT assay Antiproliferative activity against human HCT116 cells by MTT assay	[PMID: 21570843]
HCT-116	IC₅₀	5.92 μM Compound: Lapatinib	Cytotoxicity against human HCT116 cells after 24 hrs by SRB assay Cytotoxicity against human HCT116 cells after 24 hrs by SRB assay	[PMID: 30096580]
HCT-116	IC₅₀	5.92 μM Compound: Lapatinib	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by SRB assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by SRB assay	[PMID: 32361329]
HCT-116	IC₅₀	6.2 μM Compound: Lapatinib	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 28092860]
HEK-293T	CC₅₀	123.17 μM Compound: Lapatinib	Cytotoxicity against human HEK293T cells for 24 hrs by MTT assay Cytotoxicity against human HEK293T cells for 24 hrs by MTT assay	[PMID: 26652482]
HeLa	IC₅₀	0.12 μM Compound: Lapatinib	Antiproliferative activity against human HeLa cells after 12 hrs by MTT assay Antiproliferative activity against human HeLa cells after 12 hrs by MTT assay	[PMID: 26652482]
HeLa	IC₅₀	5.9 μM Compound: 5, GW-572016	Cytotoxicity against human HeLa cells overexpressing HDAC by resazurin dye reduction assay Cytotoxicity against human HeLa cells overexpressing HDAC by resazurin dye reduction assay	[PMID: 21080629]
Hep 3B2	IC₅₀	5.49 μM Compound: lapatinib	Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay	[PMID: 20143778]
HepG2	IC₅₀	0.27 μM Compound: Lapatinib	Antiproliferative activity against human HepG2 cells after 12 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 12 hrs by MTT assay	[PMID: 26652482]
HepG2	IC₅₀	11.71 μM Compound: Lapatinib	Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay	[PMID: 30096580]
HepG2	IC₅₀	11.71 μM Compound: Lapatinib	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by SRB assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by SRB assay	[PMID: 32361329]
HepG2	IC₅₀	6.27 μM Compound: lapatinib	Antiproliferative activity against human HepG2 cells after hrs by ATP content assay Antiproliferative activity against human HepG2 cells after hrs by ATP content assay	[PMID: 20143778]
HN5	IC₅₀	0.01 μM Compound: Lapatinib	Inhibition of EGF-induced EGFR phosphorylation at Tyr-residue in human HN5 cells preincubated for 24 hrs followed by EGF-stimulation and measured after 15 mins by Western blot analysis Inhibition of EGF-induced EGFR phosphorylation at Tyr-residue in human HN5 cells preincubated for 24 hrs followed by EGF-stimulation and measured after 15 mins by Western blot analysis	[PMID: 30600149]
HN5	IC₅₀	0.12 μM Compound: 1, GW-572016	Inhibition of HN5 cell growth after 72 hrs Inhibition of HN5 cell growth after 72 hrs	[PMID: 16777410]
HS27	IC₅₀	> 10000 nM Compound: 3	Cytotoxicity against human HS27 cells after 72 hrs by SRB assay Cytotoxicity against human HS27 cells after 72 hrs by SRB assay	[PMID: 19888761]
HT-29	IC₅₀	12.67 μM Compound: Lapatinib	Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 31655429]
HT-29	IC₅₀	4.62 μM Compound: 5, Tykerb	Cytotoxicity against human HT-29 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human HT-29 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
HT-29	IC₅₀	6.81 μM Compound: Lapatinib	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs under normoxia condition by SRB assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs under normoxia condition by SRB assay	[PMID: 32739648]
HT-29	IC₅₀	8.85 μM Compound: Lapatinib	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs under hypoxia condition by SRB assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs under hypoxia condition by SRB assay	[PMID: 32739648]
HUVEC	IC₅₀	47.31 μM Compound: Lapatinib	Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay	[PMID: 34435487]
JeKo-1	GI₅₀	5 μM Compound: Lapatinib	Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
JIMT-1	IC₅₀	> 10000 nM Compound: 1	Cytotoxicity against human JIMT1 cells expressing low HER-2 after 72 hrs by SRB assay Cytotoxicity against human JIMT1 cells expressing low HER-2 after 72 hrs by SRB assay	[PMID: 22372864]
K562	GI₅₀	5.7 μM Compound: Lapatinib	Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	[PMID: 29089259]
KB	IC₅₀	0.062 μM Compound: Lapatinib	Inhibition of EGFR in human KB cells assessed as reduction in EGF-stimulated EGFR phosphorylation preincubated for 1 hr followed by EGF stimulation and measured after 6 mins by ELISA Inhibition of EGFR in human KB cells assessed as reduction in EGF-stimulated EGFR phosphorylation preincubated for 1 hr followed by EGF stimulation and measured after 6 mins by ELISA	[PMID: 32139324]
KG-1a	IC₅₀	9.76 μM Compound: Lapatinib	Antiproliferative activity against human KG1a cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human KG1a cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
L929	IC₅₀	2.05 μM Compound: Lapatinib	Cytotoxicity against mouse L929 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against mouse L929 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 30508379]
LNCaP	IC₅₀	3.68 μM Compound: 5, Tykerb	Cytotoxicity against human LNCAP cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human LNCAP cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
MCF7	IC₅₀	0.011 μM Compound: Lapatinib	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay	[PMID: 25151582]
MCF7	IC₅₀	0.47 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells after 12 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 12 hrs by MTT assay	[PMID: 26652482]
MCF7	IC₅₀	12.62 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34435487]
MCF7	IC₅₀	15.71 μM Compound: lapatinib	Cytotoxicity against human MCF7 cells expressing pcDNA3 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay Cytotoxicity against human MCF7 cells expressing pcDNA3 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay	[PMID: 24355130]
MCF7	IC₅₀	15.79 μM Compound: lapatinib	Cytotoxicity against human MCF7 cells expressing HER2 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay Cytotoxicity against human MCF7 cells expressing HER2 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay	[PMID: 24355130]
MCF7	IC₅₀	19.22 μM Compound: lapatinib	Cytotoxicity against human MCF7 cells expressing HER2delta16 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay Cytotoxicity against human MCF7 cells expressing HER2delta16 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay	[PMID: 24355130]
MCF7	IC₅₀	21 nM Compound: Lapatinib	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 33545637]
MCF7	IC₅₀	4.691 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 30792101]
MCF7	IC₅₀	4.83 μM Compound: 5, Tykerb	Cytotoxicity against human MCF7 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human MCF7 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
MCF7	IC₅₀	5.02 μM Compound: Lapatinib	Cytotoxicity against human MCF7 cells after 24 hrs by SRB assay Cytotoxicity against human MCF7 cells after 24 hrs by SRB assay	[PMID: 30096580]
MCF7	IC₅₀	5.02 μM Compound: Lapatinib	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by SRB assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by SRB assay	[PMID: 32361329]
MCF7	IC₅₀	6.301 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay	[PMID: 33314925]
MCF7	IC₅₀	6.6 μM Compound: lapatinib	Antiproliferative activity against human MCF7 cells after hrs by ATP content assay Antiproliferative activity against human MCF7 cells after hrs by ATP content assay	[PMID: 20143778]
MCF7	IC₅₀	6.8 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 31655429]
MCF7	IC₅₀	6.8 μM Compound: Lapatinib	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 29684708]
MCF7	GI₅₀	8.1 μM Compound: Lapatinib	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	[PMID: 29089259]
MCF7	IC₅₀	8468 nM Compound: Lapatinib	Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
MCF7	IC₅₀	95 μM Compound: Tykerb(R)	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31125894]
MDA-MB-231	IC₅₀	> 100 μM Compound: Lapatinib	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
MDA-MB-231	IC₅₀	10.373 μM Compound: Lapatinib	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay	[PMID: 33314925]
MDA-MB-231	IC₅₀	10.6 μM Compound: Lapatinib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs	[PMID: 33139111]
MDA-MB-231	GI₅₀	20 μM Compound: Lapatinib	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MDA-MB-231	IC₅₀	29.39 μM Compound: Lapatinib	Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay	[PMID: 34435487]
MDA-MB-231	IC₅₀	30.78 μM Compound: Lapatinib	Antiproliferative activity against drug-tolerant human MDA-MB-231/lapatinib cells assessed as CD44-positive cells measured after 24 hrs by MTT assay Antiproliferative activity against drug-tolerant human MDA-MB-231/lapatinib cells assessed as CD44-positive cells measured after 24 hrs by MTT assay	[PMID: 34435487]
MDA-MB-231	IC₅₀	4.691 μM Compound: Lapatinib	Antiproliferative activity against human MDA231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA231 cells after 72 hrs by MTT assay	[PMID: 30792101]
MDA-MB-231	IC₅₀	5.4 μM Compound: lapatinib	Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay	[PMID: 20143778]
MDA-MB-231	IC₅₀	5.86 μM Compound: Lapatinib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34435487]
MDA-MB-231	IC₅₀	7.7 μM Compound: 5, Tykerb	Cytotoxicity against human MDA231 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human MDA231 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
MDA-MB-361	IC₅₀	1029 nM Compound: 1	Cytotoxicity against ER activated human MDA-MB-361 cells expressing Her-2, Src and PIK3CA mutant after 72 hrs by SRB assay Cytotoxicity against ER activated human MDA-MB-361 cells expressing Her-2, Src and PIK3CA mutant after 72 hrs by SRB assay	[PMID: 22372864]
MDA-MB-453	IC₅₀	0.19 μM Compound: Lapatinib	Cytotoxicity against human MDA-MB-453 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human MDA-MB-453 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
MDA-MB-453	IC₅₀	555 nM Compound: 1	Cytotoxicity against PTEN-deficient human MDA-MB-453 cells expressing HER-2, and PIK3CA mutant after 72 hrs by SRB assay Cytotoxicity against PTEN-deficient human MDA-MB-453 cells expressing HER-2, and PIK3CA mutant after 72 hrs by SRB assay	[PMID: 22372864]
MDA-MB-468	IC₅₀	20 μM Compound: Lapatinib	Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by MTT assay	[PMID: 28092860]
MDA-MB-468	IC₅₀	23.46 μM Compound: 3	Antiproliferative activity against EGFR overexpressing human MDA-MB-468 cells by MTT assay Antiproliferative activity against EGFR overexpressing human MDA-MB-468 cells by MTT assay	[PMID: 21570843]
MEXF276L	IC₅₀	11.37 μM Compound: 5, Tykerb	Cytotoxicity against human MEXF 276L cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human MEXF 276L cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
MIA PaCa-2	GI₅₀	10 μM Compound: Lapatinib	Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MKN-45	IC₅₀	11.48 μM Compound: 5, Tykerb	Cytotoxicity against human MKN45 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human MKN45 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
MRC5	IC₅₀	> 100 μM Compound: Lapatinib	Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
MRC5	IC₅₀	13.66 μM Compound: Lapatinib	Cytotoxicity against human MRC5 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human MRC5 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 31655429]
MV4-11	GI₅₀	10 μM Compound: Lapatinib	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
NCI-H1975	IC₅₀	> 1000 nM Compound: 3	Cytotoxicity against human NCI-H1975 cells after 24 hrs by MTT assay Cytotoxicity against human NCI-H1975 cells after 24 hrs by MTT assay	[PMID: 19888761]
NCI-H1975	IC₅₀	> 1000 nM Compound: 1	Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant after 72 hrs by SRB assay Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant after 72 hrs by SRB assay	[PMID: 22372864]
NCI-H1975	IC₅₀	12.68 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay	[PMID: 31202990]
NCI-H1975	IC₅₀	12.68 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay	[PMID: 29421573]
NCI-H1975	IC₅₀	7.25 μM Compound: 3; GW-572016	Antiproliferative activity against human NCI-H1975 expressing EGFR T790M/L858R mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human NCI-H1975 expressing EGFR T790M/L858R mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 27769671]
NCI-H1975	IC₅₀	7.37 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32139324]
NCI-H1975	IC₅₀	9 μM Compound: Tykerb(R)	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31125894]
NCI-H1975	IC₅₀	9.08 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay	[PMID: 28711703]
NCI-H460	IC₅₀	> 100 μM Compound: Lapatinib	Cytotoxicity against human NCI-H460 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human NCI-H460 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
NCI-H460	IC₅₀	13.46 μM Compound: 5, Tykerb	Cytotoxicity against human H460 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human H460 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
NCI-H460	IC₅₀	8.4 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay	[PMID: 28092860]
NCI-H522	IC₅₀	6.4 μM Compound: Lapatinib	Antiproliferative activity against human NCI-H522 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H522 cells after 72 hrs by MTT assay	[PMID: 28092860]
NCI-N87	IC₅₀	0.053 μM Compound: Lapatinib	Antiproliferative activity against human NCI-N87 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-N87 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32139324]
NCI-N87	IC₅₀	0.08 μM Compound: 1, GW-572016	Inhibition of N87 cell growth after 72 hrs Inhibition of N87 cell growth after 72 hrs	[PMID: 16777410]
NCI-N87	IC₅₀	0.09 μM Compound: Lapatinib	Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue staining Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue staining	[PMID: 22101132]
NCI-N87	IC₅₀	100 nM Compound: Lapatinib	Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA	[PMID: 20346655]
NCI-N87	IC₅₀	36 nM Compound: 1	Cytotoxicity against human NCI-N87 cells expressing HER-2 after 72 hrs by SRB assay Cytotoxicity against human NCI-N87 cells expressing HER-2 after 72 hrs by SRB assay	[PMID: 22372864]
NIH3T3	IC₅₀	4.3 μM Compound: 3	Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs by MTT assay Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs by MTT assay	[PMID: 22595177]
OVCAR-3	IC₅₀	13.44 μM Compound: 5, Tykerb	Cytotoxicity against human OVCAR3 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human OVCAR3 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
PANC-1	IC₅₀	8.12 μM Compound: 5, Tykerb	Cytotoxicity against human PANC1 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human PANC1 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
PBMC	IC₅₀	28 μM Compound: lapatinib	Cytotoxicity against human PBMC assessed as induction of cell death by cell Titer-Glo assay Cytotoxicity against human PBMC assessed as induction of cell death by cell Titer-Glo assay	[PMID: 29909341]
PC-3M	IC₅₀	4.55 μM Compound: 5, Tykerb	Cytotoxicity against human PC3M cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human PC3M cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
RAW264.7	EC₅₀	11 μM Compound: 1	Antileishmanial activity against luciferase-expressing Leishmania major amastigotes infected in mouse RAW264.7 cells after 96 hrs by luminescence assay Antileishmanial activity against luciferase-expressing Leishmania major amastigotes infected in mouse RAW264.7 cells after 96 hrs by luminescence assay	[PMID: 28337329]
RKO	IC₅₀	5.35 μM Compound: 5, Tykerb	Cytotoxicity against human RKO cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human RKO cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
SAOS-2	IC₅₀	9.38 μM Compound: 5, Tykerb	Cytotoxicity against human Saos2 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human Saos2 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
SK-BR-3	IC₅₀	0.002 μM Compound: 5, GW-572016	Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay	[PMID: 21080629]
SK-BR-3	IC₅₀	0.017 μM Compound: GW-572016	Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay	[PMID: 19028425]
SK-BR-3	IC₅₀	0.04 μM Compound: lapatinib	Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay	[PMID: 20143778]
SK-BR-3	IC₅₀	0.06 μM Compound: 3; GW-572016	Antiproliferative activity against human SK-BR-3 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human SK-BR-3 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 27769671]
SK-BR-3	IC₅₀	0.49 μM Compound: Lapatinib	Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay	[PMID: 27187856]
SK-BR-3	IC₅₀	29 nM Compound: 1	Cytotoxicity against human SKBR3 cells overexpressing HER-2 gene after 72 hrs by SRB assay Cytotoxicity against human SKBR3 cells overexpressing HER-2 gene after 72 hrs by SRB assay	[PMID: 22372864]
SK-BR-3	IC₅₀	29 nM Compound: 3	Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay	[PMID: 19888761]
SK-BR-3	IC₅₀	30.1 nM Compound: Lapatinib	Cytotoxicity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
SK-BR-3	IC₅₀	4.35 μM Compound: 3	Antiproliferative activity against ErbB2 overexpressing human SK-BR-3 cells by MTT assay Antiproliferative activity against ErbB2 overexpressing human SK-BR-3 cells by MTT assay	[PMID: 21570843]
SK-BR-3	IC₅₀	4.4 μM Compound: Lapatinib	Antiproliferative activity against human SK-BR-3 cells after 72 hrs by MTT assay Antiproliferative activity against human SK-BR-3 cells after 72 hrs by MTT assay	[PMID: 28092860]
SK-BR-3	IC₅₀	5.05 μM Compound: Lapatinib, Tykerb	Antiproliferative activity against human estrogen receptor and progesterone receptor deficient SKBR3 cells expressing HER2 after 72 hrs by MTT assay Antiproliferative activity against human estrogen receptor and progesterone receptor deficient SKBR3 cells expressing HER2 after 72 hrs by MTT assay	[PMID: 23927972]
SK-BR-3	IC₅₀	9.76 μM Compound: Lapatinib	Antiproliferative activity against human SKBR3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human SKBR3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
SK-HEP1	IC₅₀	5.3 μM Compound: lapatinib	Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay	[PMID: 20143778]
SK-MEL19	GI₅₀	5 μM Compound: Lapatinib	Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SK-OV-3	IC₅₀	0.003 μM Compound: 5, GW-572016	Cytotoxicity against human SKOV3 cells overexpressing HER2 by resazurin dye reduction assay Cytotoxicity against human SKOV3 cells overexpressing HER2 by resazurin dye reduction assay	[PMID: 21080629]
SK-OV-3	IC₅₀	0.59 μM Compound: Lapatinib	Cytotoxicity against human SKOV3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay Cytotoxicity against human SKOV3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	[PMID: 25305330]
SK-OV-3	IC₅₀	2.99 μM Compound: Lapatinib	Cytotoxicity against human SKOV3 cells overexpressing ErbB2 after 72 hrs by MTT assay Cytotoxicity against human SKOV3 cells overexpressing ErbB2 after 72 hrs by MTT assay	[PMID: 22182581]
SUM-159-PT	IC₅₀	9.76 μM Compound: Lapatinib	Antiproliferative activity against human SUM159 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human SUM159 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
SW480	IC₅₀	12.58 μM Compound: Lapatinib	Antiproliferative activity against human SW480 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human SW480 cells incubated for 72 hrs by MTT assay	[PMID: 31202990]
SW480	IC₅₀	12.58 μM Compound: Lapatinib	Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 29421573]
SW480	IC₅₀	12.58 μM Compound: Lapatinib	Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 28711703]
SW480	IC₅₀	12.58 μM Compound: Lapatinib	Antiproliferative activity against human SW480 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human SW480 cells assessed as cell growth inhibition by MTT assay	[PMID: 32739648]
T-24	IC₅₀	9.65 μM Compound: 5, Tykerb	Cytotoxicity against human BXF T24 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human BXF T24 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
T47D	IC₅₀	> 10 μM Compound: Lapatinib, Tykerb	Antiproliferative activity against human HER2 deficient T47D cells expressing estrogen receptor and progesterone receptor after 72 hrs by MTT assay Antiproliferative activity against human HER2 deficient T47D cells expressing estrogen receptor and progesterone receptor after 72 hrs by MTT assay	[PMID: 23927972]
T47D	GI₅₀	40 μM Compound: Lapatinib	Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
TE-671	IC₅₀	10.95 μM Compound: 5, Tykerb	Cytotoxicity against human TE671 cells after 4 days by propidium iodide staining-based fluorometric analysis Cytotoxicity against human TE671 cells after 4 days by propidium iodide staining-based fluorometric analysis	[PMID: 22169601]
U-87MG ATCC	GI₅₀	10 μM Compound: Lapatinib	Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
WI-38	IC₅₀	> 10 μM Compound: GW-572016	Cytotoxicity against human WI38 cells after 72 hrs by SRB assay Cytotoxicity against human WI38 cells after 72 hrs by SRB assay	[PMID: 19028425]
WI-38	IC₅₀	45.2 nM Compound: Lapatinib	Cytotoxicity against human WI-38 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human WI-38 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 33545637]

In Vitro

Lapatinib (GW2016; 0.03-10 μM; 6 hours; BT474 and HN5 cells) treatment inhibits receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was inhibited by GW2016 in a dose-dependent manner^[1].
Lapatinib (GW2016; 72 hours; HN5, A-43, BT474, N87, and CaLu-3 cells) treatment has a selective inhibition of the proliferation of human tumor cell lines^[1].
Lapatinib (GW2016; 1-10 μM; 72 hours; HN5 cells) treatment results in induces G1 arrest^[1].

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

Western Blot Analysis^[1]

Cell Line:	BT474 and HN5 cells
Concentration:	0.03 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM, or 10 µM
Incubation Time:	6 hours
Result:	Inhibited receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was also inhibited in a dose-dependent manner.

Cell Proliferation Assay^[1]

Cell Line:	HN5, A-43, BT474, N87, and CaLu-3 cells
Concentration:
Incubation Time:	72 hours
Result:	Inhibited the growth of tumor cells overexpressing EGFR or ErbB-2.

Cell Cycle Analysis^[1]

Cell Line:	HN5 cells
Concentration:	1 µM, or 10 µM
Incubation Time:	72 hours
Result:	Resulted in induction of G1 arrest.

In Vivo

Lapatinib (GW2016; 30-100 mg/kg; oral administration; twice daily; for 21 days; CD-1 nude female mice) treatment inhibits tumor xenograft growth of the HN5 cells in a dose-responsive manner at 30 and 100 mg/kg, with complete inhibition of tumor growth at the higher dose^[1].

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

Animal Model:	CD-1 nude female mice (4-6 weeks old) with HN5 cells^[1]
Dosage:	30 mg/kg, 100 mg/kg
Administration:	Oral administration; twice daily; for 21 days
Result:	Inhibited tumor xenograft growth of the HN5 cells in a dose-responsive manner.

Clinical Trial

Molecular Weight

581.06

Formula

C₂₉H₂₆ClFN₄O₄S

CAS No.

231277-92-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=S(CCNCC1=CC=C(C2=CC=C3C(C(NC4=CC(Cl)=C(C=C4)OCC5=CC(F)=CC=C5)=NC=N3)=C2)O1)(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (215.12 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	1.7210 mL	8.6050 mL	17.2099 mL
5 mM	0.3442 mL	1.7210 mL	3.4420 mL
10 mM	0.1721 mL	0.8605 mL	1.7210 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.30 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.58 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 12% SBE-β-CD in Saline
Solubility: 5 mg/mL (8.60 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

Purity: 99.83%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (247 KB) HNMR (197 KB) LCMS (475 KB)

Handling Instructions (2659 KB)

References

[1]. Rusnak DW, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94 [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.7210 mL	8.6050 mL	17.2099 mL	43.0248 mL
	5 mM	0.3442 mL	1.7210 mL	3.4420 mL	8.6050 mL
	10 mM	0.1721 mL	0.8605 mL	1.7210 mL	4.3025 mL
	15 mM	0.1147 mL	0.5737 mL	1.1473 mL	2.8683 mL
	20 mM	0.0860 mL	0.4302 mL	0.8605 mL	2.1512 mL
	25 mM	0.0688 mL	0.3442 mL	0.6884 mL	1.7210 mL
	30 mM	0.0574 mL	0.2868 mL	0.5737 mL	1.4342 mL
	40 mM	0.0430 mL	0.2151 mL	0.4302 mL	1.0756 mL
	50 mM	0.0344 mL	0.1721 mL	0.3442 mL	0.8605 mL
	60 mM	0.0287 mL	0.1434 mL	0.2868 mL	0.7171 mL
	80 mM	0.0215 mL	0.1076 mL	0.2151 mL	0.5378 mL
	100 mM	0.0172 mL	0.0860 mL	0.1721 mL	0.4302 mL

Lapatinib Related Classifications

Help & FAQs

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:

Lapatinib231277-92-2GW572016 GW2016GW 572016GW-572016GW2016GW 2016GW-2016EGFRAutophagyFerroptosisEpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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Lapatinib (Synonyms: GW572016; GW2016)

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