ABT-737
ABT-737 is a BH3 mimetic that acts as an inhibitor of Bcl-2, Bxl-xl, and Bcl-ω. ABT-737 exhibits anticancer chemotherapeutic and antithrombotic activities. ABT-737 is currently in clinical trials as one component of a combination therapy in the treatment of various cancers such as acute myelogenous leukemia (AML). This compound inhibits growth of AML cells in vitro and increases survival rates and lifespan in animal models of AML. In vitro, ABT-737 induces mitochondrial membrane depolarization in platelets, inducing apoptosis and clearance.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18835058
| Cas No. |
852808-04-9 |
|---|---|
| Purity |
≥98% |
| Formula |
C42H45ClN6O5S2 |
| Formula Wt. |
813.43 |
| Synonym |
ABT737 |
| Appearance |
Yellow powder |
Lieber J, Armeanu-Ebinger S, Fuchs J. The Role of BH3-Mimetic Drugs in the Treatment of Pediatric Hepatoblastoma. Int J Mol Sci. 2015 Feb 16;16(2):4190-4208. PMID: 25690034.
Baev DV, Krawczyk J, O’Dwyer M, et al. The BH3-mimetic ABT-737 effectively kills acute myeloid leukemia initiating cells. Leuk Res Rep. 2014 Sep 1;3(2):79-82. PMID: 25379408.
Gyulkhandanyan AV, Mutlu A, Allen DJ, et al. BH3-mimetic ABT-737 induces strong mitochondrial membrane depolarization in platelets but only weakly stimulates apoptotic morphological changes, platelet shrinkage and microparticle formation. Thromb Res. 2014 Jan;133(1):73-9. PMID: 24268298.
Beurlet S, Omidvar N, Gorombei P, et al. BCL-2 inhibition with ABT-737 prolongs survival in an NRAS/BCL-2 mouse model of AML by targeting primitive LSK and progenitor cells. Blood. 2013 Oct 17;122(16):2864-76. PMID: 23943652.
