Dactolisib (Synonyms: BEZ235; NVP-BEZ235)

Name: Dactolisib
Brand: MedChemExpress
SKU: HY-50673
Rating: 5.0 (62 reviews)

Cat. No.: HY-50673 Purity: 99.94%: FAQs
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Dactolisib (BEZ235) is an orally active and dual pan-class I PI3K and mTOR kinase inhibitor with IC₅₀s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2.

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

Dactolisib Chemical Structure

CAS No. : 915019-65-7

Size	Price	Stock	Quantity
50 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 106	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 172	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 343	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 62 publication(s) in Google Scholar

Other Forms of Dactolisib:

Dactolisib Tosylate In-stock

57 Publications Citing Use of MCE Dactolisib

: Dactolisib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 9;37(1):188. [Abstract]; Representative images of the western blotting analysis of TSSC3, ATG5, P62, LC3, Src, Akt, mTOR and their phosphorylated versions in MTF and SaOS2 cells. Cells are treated with TSSC3-overexpression, IGF-1, p-YEEI, and BEZ235 separately or in combination.

: Dactolisib purchased from MedChemExpress. Usage Cited in: Biomed Res Int. 2018 Aug 5;2018:8372085. [Abstract]; Changes of p-AKT and p-p70 S6K proteins after treatment with NVP-BEZ235 in Ishikawa and Ishikawa-TAX cells. Changes of p-AKT and p-p70 S6K proteins after treatment of Ishikawa and Ishikawa-TAX cells with NVP-BEZ235.

: Dactolisib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617. [Abstract]; Immunoblot analysis of KRAS protein levels in parental (P) and resistant derivatives (R1 and R2) following 4 h treatment with the corresponding inhibitors Rapamycin, AZD2014, MLN0128, BEZ235 and 4EGI-1. Images are cropped for clarity from the same exposure of the same membrane.

: Dactolisib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jul 11;8(28):45470-45483. [Abstract]; Activity of PI3K/AKT/mTOR is monitored by examining phosphorylation of AKT-S473, AKT-T308, and S6 by western blotting.

: Dactolisib purchased from MedChemExpress. Usage Cited in: Leukemia. 2014 Sep;28(9):1819-27. [Abstract]; Western blot analysis of human T-ALL cell lines treated for 24 hours using DMSO (vehicle control), 1 μM JQ1, 500 nM BEZ235, or both drugs in combination, using the indicated antibodies. Western blot analysis of these T-ALL cell lines following treatment with JQ1, BEZ235 or both drugs in combination reveals cooperative upregulation of BIM protein expression coupled to induction of apoptosis, as assessed by PARP cleavage.

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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mTOR mTORC1 mTORC2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

p110α

4 nM (IC₅₀)

p110α-H1047R

4.6 nM (IC₅₀)

p110α-E545K

5.7 nM (IC₅₀)

p110γ

5 nM (IC₅₀)

p110δ

7 nM (IC₅₀)

p110β

75 nM (IC₅₀)

mTOR

20.7 nM (IC₅₀)

mTORC1

mTORC2

Autophagy

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.58 μM Compound: BEZ235	Antiproliferative activity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]
A-431	IC₅₀	12.5 μM Compound: BEZ-235	Cytotoxicity against human A431 cells after 24 hrs by MTT assay Cytotoxicity against human A431 cells after 24 hrs by MTT assay	[PMID: 25062005]
A549	IC₅₀	0.1 μM Compound: BEZ235	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: 24878359]
A549	IC₅₀	0.28 μM Compound: BEZ235	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 26210161]
A549	IC₅₀	0.38 μM Compound: BEZ235	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31446244]
A549	IC₅₀	0.62 μM Compound: Dactolisib	Cytotoxicity against human A549 cells after 72 hrs by SRB assay Cytotoxicity against human A549 cells after 72 hrs by SRB assay	[PMID: 29407971]
A549	IC₅₀	0.62 μM Compound: BEZ235	Antiproliferative activity against human A549 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human A549 cells after 72 hrs by sulforhodamine B assay	[PMID: 29475582]
A549	IC₅₀	0.76 μM Compound: BEZ235	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: 26321603]
A549	IC₅₀	1.08 μM Compound: BEZ235	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]
A549	IC₅₀	6.5 μM Compound: BEZ-235	Cytotoxicity against human A549 cells after 24 hrs by MTT assay Cytotoxicity against human A549 cells after 24 hrs by MTT assay	[PMID: 25062005]
A549	IC₅₀	6.5 μM Compound: BEZ-235	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 25088398]
BT-549	IC₅₀	0.74 μM Compound: Dactolisib	Cytotoxicity against human BT549 cells after 72 hrs by SRB assay Cytotoxicity against human BT549 cells after 72 hrs by SRB assay	[PMID: 29407971]
COLO 205	IC₅₀	0.085 μM Compound: BEZ-235	Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay	[PMID: 25062005]
COLO 205	IC₅₀	0.085 μM Compound: BEZ-235	Cytotoxicity against human COLO205 cells after 48 hrs by MTT assay Cytotoxicity against human COLO205 cells after 48 hrs by MTT assay	[PMID: 25088398]
HCC827	IC₅₀	0.53 μM Compound: BEZ235	Antiproliferative activity against human HCC827 cells assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis Antiproliferative activity against human HCC827 cells assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis	[PMID: 34403956]
HCT-116	IC₅₀	0.044 μM Compound: BEZ-235	Cytotoxicity against human HCT116 cells after 24 hrs by MTT assay Cytotoxicity against human HCT116 cells after 24 hrs by MTT assay	[PMID: 25062005]
HCT-116	IC₅₀	0.044 μM Compound: BEZ-235	Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 25088398]
HCT-116	IC₅₀	0.14 μM Compound: 1; BEZ-235	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay	10.1039/C5MD00401B
HCT-116	IC₅₀	0.2 μM Compound: BEZ-235	Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 26596710]
HCT-116	IC₅₀	0.22 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 28109945]
HCT-116	IC₅₀	0.24 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31446244]
HCT-116	IC₅₀	0.29 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay	[PMID: 26321603]
HCT-116	IC₅₀	0.29 μM Compound: BEZ235	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 26210161]
HCT-116	IC₅₀	0.3 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells by MTT assay Antiproliferative activity against human HCT116 cells by MTT assay	[PMID: 31434616]
HCT-116	IC₅₀	0.32 μM Compound: BEZ235	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: 24878359]
HCT-116	IC₅₀	0.37 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells harboring PIK3CA mutant H1047R measured after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells harboring PIK3CA mutant H1047R measured after 72 hrs by MTT assay	[PMID: 31176568]
HCT-116	IC₅₀	0.37 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells harboring PI3CA H1047R mutant after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells harboring PI3CA H1047R mutant after 72 hrs by MTT assay	[PMID: 27544401]
HCT-116	IC₅₀	0.56 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells harboring PI3CA H1047R mutant after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells harboring PI3CA H1047R mutant after 72 hrs by MTT assay	[PMID: 26652969]
HCT-116	IC₅₀	0.84 μM Compound: Dactolisib	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 29937355]
HCT-116	IC₅₀	0.84 μM Compound: Dactolisib	Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 29407971]
HCT-116	IC₅₀	0.84 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human HCT116 cells after 72 hrs by sulforhodamine B assay	[PMID: 29475582]
HCT-116	IC₅₀	1.16 μM Compound: BEZ235	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: 23871904]
HCT-116	IC₅₀	1.7 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]
HCT-15	IC₅₀	0.91 μM Compound: BEZ235	Antiproliferative activity against human HCT-15 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human HCT-15 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
HEL	IC₅₀	0.29 μM Compound: BEZ235	Antiproliferative activity against human HEL cells assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis Antiproliferative activity against human HEL cells assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis	[PMID: 34403956]
HeLa	IC₅₀	1.09 μM Compound: BEZ235	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
HeLa	IC₅₀	1.17 μM Compound: BEZ235	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]
HepG2	IC₅₀	4.04 μM Compound: BEZ235	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]
HL-60	IC₅₀	0.91 μM Compound: BEZ235	Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31446244]
HL-60	IC₅₀	1 μM Compound: 5; BEZ235	Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay	[PMID: 30077608]
HL-60	IC₅₀	12.42 μM Compound: BEZ-235	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 25088398]
HT-29	IC₅₀	1.01 μM Compound: BEZ235	Antiproliferative activity against human HT-29 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
Huh-7	IC₅₀	0.53 μM Compound: BEZ235	Antiproliferative activity against human HuH7 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HuH7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31446244]
K562	ED₅₀	0.02021 μM Compound: 3; BEZ-235	Potentiation of (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as (-)-lomaiviticin A ED50 at compound to (-)-lomaiviticin A ratio of 200:1 after 48 hrs by cell titer-glo luminescence assay (Rvb = 0.23776 nM) Potentiation of (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as (-)-lomaiviticin A ED50 at compound to (-)-lomaiviticin A ratio of 200:1 after 48 hrs by cell titer-glo luminescence assay (Rvb = 0.23776 nM)	[PMID: 27177826]
K562	ED₅₀	0.04893 μM Compound: 3; BEZ-235	Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by cell titer-glo luminescence assay Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by cell titer-glo luminescence assay	[PMID: 27177826]
K562	IC₅₀	5.7 μM Compound: 5; BEZ235	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay Antiproliferative activity against human K562 cells after 48 hrs by MTT assay	[PMID: 30077608]
MCF7	IC₅₀	0.05 μM Compound: 1; BEZ-235	Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay	10.1039/C5MD00401B
MCF7	IC₅₀	0.05 μM Compound: BEZ-235	Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay	[PMID: 26596710]
MCF7	GI₅₀	0.06 μM Compound: NVP-BEZ235; BEZ235	Growth inhibition of human MCF7 cells after 72 hrs by SRB assay Growth inhibition of human MCF7 cells after 72 hrs by SRB assay	[PMID: 28835805]
MCF7	IC₅₀	0.2 μM Compound: BEZ235	Antiproliferative activity against human MCF7 cells by MTT assay Antiproliferative activity against human MCF7 cells by MTT assay	[PMID: 31434616]
MCF7	IC₅₀	0.26 μM Compound: BEZ235	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 26210161]
MCF7	IC₅₀	0.35 μM Compound: BEZ235	Antiproliferative activity against human MCF7 cells harboring PIK3CA mutant E545K measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells harboring PIK3CA mutant E545K measured after 72 hrs by MTT assay	[PMID: 31176568]
MCF7	IC₅₀	0.35 μM Compound: BEZ235	Antiproliferative activity against human MCF7 cells harboring PI3CA E545K mutant after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells harboring PI3CA E545K mutant after 72 hrs by MTT assay	[PMID: 27544401]
MCF7	IC₅₀	0.45 μM Compound: BEZ235	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: 31228810]
MCF7	IC₅₀	0.48 μM Compound: BEZ235	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay	[PMID: 26321603]
MCF7	IC₅₀	0.55 μM Compound: BEZ235	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: 24878359]
MCF7	IC₅₀	0.73 μM Compound: BEZ235	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 23871904]
MCF7	IC₅₀	1.09 μM Compound: BEZ235	Antiproliferative activity against human MCF7 cells harboring PI3CA E545K mutant after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells harboring PI3CA E545K mutant after 72 hrs by MTT assay	[PMID: 26652969]
MCF7	IC₅₀	1.33 μM Compound: Dactolisib	Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay	[PMID: 29407971]
MCF7	IC₅₀	1.33 μM Compound: BEZ235	Antiproliferative activity against human MCF7 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human MCF7 cells after 72 hrs by sulforhodamine B assay	[PMID: 29475582]
MDA-MB-231	IC₅₀	0.18 μM Compound: BEZ235	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay	[PMID: 29475582]
MDA-MB-231	IC₅₀	0.56 μM Compound: Dactolisib	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay	[PMID: 29937355]
NCI-H23	IC₅₀	1 μM Compound: BEZ235	Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28038940]
NCI-H3122	IC₅₀	0.96 μM Compound: BEZ235	Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
NCI-H446	IC₅₀	0.87 μM Compound: BEZ235	Antiproliferative activity against PTEN-null human NCI-H446 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against PTEN-null human NCI-H446 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
NCI-H460	GI₅₀	0.61 μM Compound: NVP-BEZ235; BEZ235	Growth inhibition of human NCI-H460 cells after 72 hrs by SRB assay Growth inhibition of human NCI-H460 cells after 72 hrs by SRB assay	[PMID: 28835805]
PC-3	IC₅₀	0.19 μM Compound: 1; BEZ-235	Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay	10.1039/C5MD00401B
PC-3	IC₅₀	0.21 μM Compound: BEZ-235	Cytotoxicity against human PC3 cells after 72 hrs by SRB assay Cytotoxicity against human PC3 cells after 72 hrs by SRB assay	[PMID: 26596710]
PC-3	IC₅₀	0.51 μM Compound: BEZ235	Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay	[PMID: 28109945]
PC-3	IC₅₀	12.3 μM Compound: BEZ-235	Cytotoxicity against human PC3 cells after 24 hrs by MTT assay Cytotoxicity against human PC3 cells after 24 hrs by MTT assay	[PMID: 25062005]
PC-3	IC₅₀	12.3 μM Compound: BEZ-235	Cytotoxicity against human PC3 cells after 48 hrs by MTT assay Cytotoxicity against human PC3 cells after 48 hrs by MTT assay	[PMID: 25088398]
Raji	IC₅₀	0.22 μM Compound: 4; BEZ235	Antiproliferative activity against human Raji cells after 48 hrs by CCK8 assay Antiproliferative activity against human Raji cells after 48 hrs by CCK8 assay	[PMID: 30605829]
Raji	IC₅₀	0.3 μM Compound: BEZ235	Antiproliferative activity against human Raji cells assessed as inhibition of cell growth after 48 hrs by MTT assay Antiproliferative activity against human Raji cells assessed as inhibition of cell growth after 48 hrs by MTT assay	[PMID: 32987316]
Raji	IC₅₀	0.52 μM Compound: BEZ235	Antiproliferative activity against human Raji cells by MTT assay Antiproliferative activity against human Raji cells by MTT assay	[PMID: 31434616]
Raji	IC₅₀	4.3 μM Compound: 5; BEZ235	Antiproliferative activity against human Raji cells after 48 hrs by MTT assay Antiproliferative activity against human Raji cells after 48 hrs by MTT assay	[PMID: 30077608]
Ramos	IC₅₀	0.0068 μM Compound: 4; BEZ235	Antiproliferative activity against human Ramos cells after 48 hrs by CCK8 assay Antiproliferative activity against human Ramos cells after 48 hrs by CCK8 assay	[PMID: 30605829]
Ramos	IC₅₀	0.4 μM Compound: BEZ235	Antiproliferative activity against human Ramos cells by MTT assay Antiproliferative activity against human Ramos cells by MTT assay	[PMID: 31434616]
Ramos	IC₅₀	0.6 μM Compound: BEZ235	Antiproliferative activity against human Ramos cells assessed as inhibition of cell growth after 48 hrs by MTT assay Antiproliferative activity against human Ramos cells assessed as inhibition of cell growth after 48 hrs by MTT assay	[PMID: 32987316]
SH-SY5Y	IC₅₀	0.79 μM Compound: BEZ235	Antiproliferative activity against human SH-SY5Y assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis Antiproliferative activity against human SH-SY5Y assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis	[PMID: 34403956]
SK-HEP1	IC₅₀	1.82 μM Compound: Dactolisib	Cytotoxicity against human SKHEP1 cells after 72 hrs by SRB assay Cytotoxicity against human SKHEP1 cells after 72 hrs by SRB assay	[PMID: 29407971]
SK-HEP1	IC₅₀	1.82 μM Compound: BEZ235	Antiproliferative activity against human SKHEP1 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human SKHEP1 cells after 72 hrs by sulforhodamine B assay	[PMID: 29475582]
SNU-638	IC₅₀	1.24 μM Compound: Dactolisib	Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay	[PMID: 29937355]
SNU-638	IC₅₀	1.24 μM Compound: Dactolisib	Cytotoxicity against human SNU638 cells after 72 hrs by SRB assay Cytotoxicity against human SNU638 cells after 72 hrs by SRB assay	[PMID: 29407971]
SNU-638	IC₅₀	1.24 μM Compound: BEZ235	Antiproliferative activity against human SNU638 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human SNU638 cells after 72 hrs by sulforhodamine B assay	[PMID: 29475582]
SU-DHL-6	IC₅₀	0.07 μM Compound: BEZ235	Antiproliferative activity against human SUDHL6 cells measured after 72 hrs by CCK-8 assay Antiproliferative activity against human SUDHL6 cells measured after 72 hrs by CCK-8 assay	[PMID: 31176568]
SW-620	IC₅₀	0.87 μM Compound: BEZ235	Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
T47D	GI₅₀	0.3 μM Compound: NVP-BEZ235; BEZ235	Growth inhibition of human T47D cells after 72 hrs by SRB assay Growth inhibition of human T47D cells after 72 hrs by SRB assay	[PMID: 28835805]
T47D	IC₅₀	11.2 μM Compound: BEZ-235	Cytotoxicity against human T47D cells after 24 hrs by MTT assay Cytotoxicity against human T47D cells after 24 hrs by MTT assay	[PMID: 25062005]
U-87MG ATCC	IC₅₀	0.16 μM Compound: NVP-BEZ235	Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 72 hrs by Z2 coulter counter method Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 72 hrs by Z2 coulter counter method	[PMID: 27081742]
U-87MG ATCC	GI₅₀	0.28 μM Compound: NVP-BEZ235; BEZ235	Growth inhibition of human U87MG cells after 72 hrs by SRB assay Growth inhibition of human U87MG cells after 72 hrs by SRB assay	[PMID: 28835805]
U-87MG ATCC	IC₅₀	0.6 μM Compound: NVP-BEZ235	Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs by Z2 coulter counter method Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs by Z2 coulter counter method	[PMID: 27081742]
U-87MG ATCC	IC₅₀	0.77 μM Compound: BEZ235	Cytotoxicity against human U87MG cells after 72 hrs by MTT assay Cytotoxicity against human U87MG cells after 72 hrs by MTT assay	[PMID: 26210161]
U-87MG ATCC	IC₅₀	1.32 μM Compound: BEZ235	Antiproliferative activity against human U87MG cells after 48 hrs by MTT assay Antiproliferative activity against human U87MG cells after 48 hrs by MTT assay	[PMID: 23871904]
U-87MG ATCC	IC₅₀	1.41 μM Compound: BEZ235	Antiproliferative activity against human U87MG cells incubated for 72 hrs by MTT assay Antiproliferative activity against human U87MG cells incubated for 72 hrs by MTT assay	[PMID: 26321603]
U-87MG ATCC	IC₅₀	2.34 μM Compound: BEZ235	Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay	[PMID: 24878359]
U-87MG ATCC	IC₅₀	824.7 μM Compound: NVP-BEZ235	Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 24 hrs by Z2 coulter counter method Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 24 hrs by Z2 coulter counter method	[PMID: 27081742]

In Vitro

Dactolisib (BEZ235) potently inhibits PI3K in an ATP Competitive Manner. Dactolisib (BEZ235) (250 nM) significantly reduced the phosphorylation levels of the mTOR activated kinase p70S6K. Dactolisib (BEZ235) also leads to a reduction of S235/S236P-RPS6 levels with an IC₅₀ of 6.5 nM, suggesting that Dactolisib (BEZ235) can directly inhibit the mTOR kinase, as the kinase domain of mTOR is highly homologous to the one of class IA PI3K. The activity of Dactolisib (BEZ235) against mTOR is confirmed using a biochemical mTOR K-LISA assay (IC₅₀, 20.7 nM)^[1].
The IC₅₀s of Dactolisib (BEZ235) for HCT116, DLD-1, and SW480 cell lines are 14.3±6.4, 9.0±1.5, and 12.0±1.6 nM, respectively^[2].

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

In Vivo

Dactolisib (BEZ235) (45 mg/kg, p.o.) treatment induces colonic tumor regression in a GEM model for sporadic PIK3CA wild-type CRC^[2]. Dactolisib (BEZ235) (45 mg/kg) is administered to MENX rats (n=2 each group) by oral gavage and animals are sacrificed 1 or 6 hours after treatment. Immunostains for P-AKT and P-S6 show considerable reduction of the two proteins, and particularly of P-S6, 6 hours after administration of Dactolisib (BEZ235) when compares with PEG-treated rats. At 6 hours after treatment, the pituitary adenomas of Dactolisib (BEZ235)-treated rats has a proteomic profile significantly different from the tumors of placebo-treated rats^[3].

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

Clinical Trial

Molecular Weight

469.54

Formula

C₃₀H₂₃N₅O

CAS No.

915019-65-7

Appearance

Solid

Color

White to light yellow

SMILES

CN(C1=C2C3=CC(C4=CC5=CC=CC=C5N=C4)=CC=C3N=C1)C(N2C6=CC=C(C=C6)C(C)(C#N)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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

5% TFA : 8.33 mg/mL (17.74 mM; ultrasonic and warming and heat to 60°C)

DMSO : 7.81 mg/mL (16.63 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMF : 2 mg/mL (4.26 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1297 mL	10.6487 mL	21.2974 mL
5 mM	0.4259 mL	2.1297 mL	4.2595 mL
10 mM	0.2130 mL	1.0649 mL	2.1297 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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: ≥ 0.52 mg/mL (1.11 mM); Clear solution

This protocol yields a clear solution of ≥ 0.52 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.2 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% Corn Oil
Solubility: ≥ 0.52 mg/mL (1.11 mM); Clear solution

This protocol yields a clear solution of ≥ 0.52 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 (5.2 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: 50% PEG300 50% Saline
Solubility: 12.5 mg/mL (26.62 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 10% 1-Methyl-2-pyrrolidinone 90% PEG300
Solubility: ≥ 1.1 mg/mL (2.34 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(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: 99.94%

Select Batch:

Data Sheet (287 KB) SDS (393 KB)

COA (257 KB) HNMR (276 KB) LCMS (273 KB) Elemental Analysis Report (115 KB)

Handling Instructions (2659 KB)

References

[1]. Maira SM, et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol Cancer Ther, 2008, 7(7), 1851-1863. [Content Brief]

[2]. Roper J, et al. The dual PI3K/mTOR inhibitor NVP-BEZ235 induces tumor regression in a genetically engineered mouse model of PIK3CA wild-type colorectal cancer. PLoS One, 2011, 6(9), e25132. [Content Brief]

[3]. Lee M, et al. Targeting PI3K/mTOR Signaling Displays Potent Antitumor Efficacy against Nonfunctioning Pituitary Adenomas. Clin Cancer Res. 2015 Jul 15;21(14):3204-15. [Content Brief]

Cell Assay ^[2]	HCT116 (PIK3CA mutant; kinase domain at H1047R), DLD-1 (PIK3CA mutant; helical domain at E545K), and SW480 (PIK3CA wild-type) human CRC cell lines (ATCC) and isogenic DLD-1 PIK3CA mutant and wild-type cells are maintained in DMEM. Cells are plated at different initial densities (HCT116: 3,000 cells/well, DLD-1: 5,500 cells/well, SW480: 4,500 cells/well, DLD-1 PIK3CA mutant: 7,000 cells/well, and DLD-1 PIK3CA wild-type: 9,000 cells/well) to account for differential growth kinetics. After 16 hours, cells are incubated with increasing concentrations of BEZ235 (10, 100, 1000 nM), and drug-containing growth medium is changed every 24 hours. Cell viability is assessed 16 hours after the initial plating and 48 hours after initiation of drug treatment using the colorimetric MTS assay CellTiter 96 AQueous One Solution Cell Proliferation Assay. Cell viability after drug treatment is normalized to that of untreated cells also grown for 48 hours. IC₅₀ values are calculated using 4 parameter nonlinear regression in GraphPad Prism 5^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]^[3]	Mice^[2] Tumor-bearing Apc CKO mice are randomly assigned to treatment with either control vehicle alone (n=8) or 45 mg/kg body weight BEZ235 in 10% 1-methyl-2-pyrrolidone/90% PEG 300 (n=8) by daily oral gavage for 28 days. The treatment dose is chosen based on literature indicating that 40-50 mg/kg body weight BEZ235 effectively treats murine tumor models without adverse effects. Base on pharmacokinetic studies demonstrating maximal tissue concentration one hour after NVP-BEZ235 administration, tumor-bearing mice are sacrificed one hour after final treatment dose. Colonic tumor volume is assessed using calipers (width×length×height) and tumors are harvested for both western blot analysis and immunohistochemistry. Rats^[3] MENX-affected rats used. Three doses of BEZ235 are tested in MENX rats: 20, 30, and 45 mg/kg. As the two higher doses causes a weight loss >10% after 10 days of treatment, the dose of 20 mg/kg is used for further studies. For MRI studies, MENX-affected rats at 7 to 8 months of age (with sizeable adenomas but still in good general health) are treated for 14 days with BEZ235 (20 mg/kg) or placebo (PEG) administered daily per oral gavage. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Maira SM, et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol Cancer Ther, 2008, 7(7), 1851-1863. [Content Brief] [2]. Roper J, et al. The dual PI3K/mTOR inhibitor NVP-BEZ235 induces tumor regression in a genetically engineered mouse model of PIK3CA wild-type colorectal cancer. PLoS One, 2011, 6(9), e25132. [Content Brief] [3]. Lee M, et al. Targeting PI3K/mTOR Signaling Displays Potent Antitumor Efficacy against Nonfunctioning Pituitary Adenomas. Clin Cancer Res. 2015 Jul 15;21(14):3204-15. [Content Brief]

Complete Stock Solution Preparation Table

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

DMF / DMSO / 5% TFA	1 mM	2.1297 mL	10.6487 mL	21.2974 mL	53.2436 mL
DMSO / 5% TFA	5 mM	0.4259 mL	2.1297 mL	4.2595 mL	10.6487 mL
	10 mM	0.2130 mL	1.0649 mL	2.1297 mL	5.3244 mL
	15 mM	0.1420 mL	0.7099 mL	1.4198 mL	3.5496 mL

Dactolisib 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:

Dactolisib915019-65-7BEZ235 NVP-BEZ235BEZ 235BEZ-235PI3KmTORAutophagyPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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Dactolisib (Synonyms: BEZ235; NVP-BEZ235)

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