Navitoclax

Research use only, not for human use.

Navitoclax (ABT-263) is a potent, orally bioavailable Bcl-2 family inhibitor with Ki of <1 nM for Bcl-2, Bcl-xL, and Bcl-w.

Navitoclax (ABT-263) is a potent, orally bioavailable Bcl-2 family inhibitor with Ki of <1 nM for Bcl-2, Bcl-xL, and Bcl-w; binds more weakly to Mcl-1 and A1 (Ki>350 nM); disrupts Bcl-2/Bcl-xL interactions with pro-death proteins (e.g., Bim), induces apoptosis, shows cellular activity against a panel of human tumor cell lines (EC50<1 uM); induces complete tumor regressions in xenograft models of NSCLA and ALL.Blood Cancer Phase 2 Clinical.

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Animal Model:Mice with NCI-H1650 modelDosage:100 mg/kg Administration:Orally; daily; for 21 consecutive days Result:As a single agent, 100 mg/kg alone dosed daily had no significant antitumor activity. Notably, the combination with OSI-744 resulted in 98% TGI and durable tumor regressions in 100% of treated tumor-bearing mice.

ABT-263 | ABT 263 | ABT263

Angiogenesis

Bcl-2

Bcl-2|Bcl-w|Bcl-xL

Cancer

Blood cancer

923564-51-6

974.6127

C47H55ClF3N5O6S3

>98% (HPLC)

10 mM in DMSO

O=C(NS(=O)(C1=CC=C(N[C@H](CCN2CCOCC2)CSC3=CC=CC=C3)C(S(=O)(C(F)(F)F)=O)=C1)=O)C4=CC=C(N5CCN(CC6=C(C7=CC=C(Cl)C=C7)CCC(C)(C)C6)CC5)C=C4

Benzamide, 4-[4-[[2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(4-morpholinyl)-1-[(phenylthio)methyl]propyl]amino]-3-[(trifluoromethyl)sulfonyl]phenyl]sulfonyl]-

(-20℃)

With Ice Pack

≥ 2 years