[CAS NO. 1257044-40-8] Venetoclax (ABT-199)

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PRODUCTS SPECIFICATIONS [1257044-40-8]

Catalog

SLK-S8048

Brand

Selleck

CAS

1257044-40-8

DESCRIPTION [1257044-40-8]

Overview

MDL	MFCD23160052
Molecular Weight	868.44
Molecular Formula	C45H50ClN7O7S
SMILES	C(C1=C(CC(C)(C)CC1)C2=CC=C(Cl)C=C2)N3CCN(CC3)C4=CC(OC=5C=C6C(=NC5)NC=C6)=C(C(NS(=O)(=O)C7=CC(N(=O)=O)=C(NCC8CCOCC8)C=C7)=O)C=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.1515 mL	5.7575 mL	11.5149 mL
5 mM	0.2303 mL	1.1515 mL	2.3030 mL
10 mM	0.1151 mL	0.5757 mL	1.1515 mL
50 mM	0.0230 mL	0.1151 mL	0.2303 mL

Description

Venetoclax (ABT-199, GDC-0199) is a -selective inhibitor with of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Venetoclax is reported to induce cell growth suppression, , cell cycle arrest, and in triple negative breast cancer MDA-MB-231 cells. Phase 3.

Features

Re-engineered version of ABT-263 (Navitoclax).

Targets

Bcl-2 ^[1]
(Cell-free assay)

<0.01 nM(Ki)

In vitro

ABT-199 shows less sensitivity to Bcl-xL, Mcl-1 and Bcl-w with K of 48 nM, > 444 nM and 245 nM, respectively. ABT-199 potently inhibits FL5.12-Bcl-2 cells, RS4;11 cells with EC50 of 4 nM and 8 nM, while shows low activity against FL5.12-Bcl-xL cells with EC50 of 261 nM. ABT-199 induces a rapid apoptosis in RS4;11 cells with cytochrome c release, caspase activation, the externalization of phosphatidylserine and the accumulation of sub-G0/G1 DNA. Quantitative immunoblotting reveals that sensitivity to ABT-199 correlated strongly with the expression of Bcl-2, including NHL, DLBCL, MCL, AML and ALL cell lines. ABT-199 also induces apoptosis in CLL with an average EC50 of 3.0 nM.

In vivo

ABT-199 (100 mg/kg) causes a maximal tumor growth inhibition of 95% and tumor growth delay of 152% in RS4;11 xenografts. ABT-199 also inhibits xenograft growth (DoHH2, Granta-519) as a single agent or in combination with SDX-105 and other agents.

References

[1] Souers AJ, et al. Nat Med, 2013, 19(2), 202-208.

Synonyms

Benzamide, 4-[4-[[2-(4-chlorophenyl)-4,4-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[3-nitro-4-[[(tetrahydro-2H-pyran-4-yl)methyl]amino]phenyl]sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-

4-[4-[[2-(4-Chlorophenyl)-4,4-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[3-nitro-4-[[(tetrahydro-2H-pyran-4-yl)methyl]amino]phenyl]sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide

ABT 199

GDC 0199

Venetoclax

Venclexta

Venclyxto

RG 7601

RG7601

RG-7601