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ABT 199
- GDC 0199 - Venetoclax- Soluble in DMSO
- MF: C45H50ClN7O7S
- MW: 868.44
Description
ABT 199 (Venetoclax) is a highly potent, orally bioavailable and BCL-2-selective inhibitor that acts as a BH3 mimetic. It promotes apoptosis in BCL-2-dependent tumor cells while reducing the thrombocytopenia liability associated with BCL-XL inhibition.
BCL-2 is a key anti-apoptotic protein that enables survival of hematologic malignancies and therapy-resistant cancer cells. ABT 199 is a clinically important reference compound for apoptosis pathway pharmacology and BCL-2 dependency studies.
Key Features
- Selective BCL-2 inhibitor
- BH3 mimetic apoptosis inducer
- Orally bioavailable oncology scaffold
- Designed to spare BCL-XL-mediated platelet toxicity
Applications
- BCL-2 dependency studies
- Apoptosis pathway research
- Leukemia and lymphoma model assays
- BH3 mimetic pharmacology profiling
More Information
| Parent CAS No. | 1257044-40-8 |
|---|---|
| Chemical Name | 2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)-N-(3-nitro-4-((tetrahydro-2H-pyran-4-yl)methylamino)phenylsulfonyl)benzamide |
| SMILES | C(NS(=O)(=O)C1C=C([N+]([O-])=O)C(NCC2CCOCC2)=CC=1)(=O)C1=C(OC2C=C3C=CNC3=NC=2)C=C(N2CCN(CC3CCC(C)(C)CC=3C3=CC=C(Cl)C=C3)CC2)C=C1 |
| MFCD | N.A. |
| InChi | InChI=1S/C45H50ClN7O7S/c1-45(2)15-11-33(39(26-45)31-3-5-34(46)6-4-31)29-51-17-19-52(20-18-51)35-7-9-38(42(24-35)60-36-23-32-12-16-47-43(32)49-28-36)44(54)50-61(57,58)37-8-10-40(41(25-37)53(55)56)48-27-30-13-21-59-22-14-30/h3-10,12,16,23-25,28,30,48H,11,13-15,17-22,26-27,29H2,1-2H3,(H,47,49)(H,50,54) |
| InChiKey | LQBVNQSMGBZMKD-UHFFFAOYSA-N |
| CID | 49846579 |
| Short Description | Bcl-2 inhibitor |
References
- AJ Souers et al. ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat. Med. 2013, 19(2), 202-208.
- C Touzeau et al. The Bcl-2 specific BH3 mimetic ABT-199: a promising targeted therapy for t(11;14) multiple myeloma. Leukemia advance online publication 16 August 2013; doi: 10.1038/leu.2013.216.
- CJ Vandenberg and S Cory. ABT-199, a new Bcl-2–specific BH3 mimetic, has in vivo efficacy against aggressive Myc-driven mouse lymphomas without provoking thrombocytopenia. Blood, 2013, 121(12), 2285-2288.
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