ABT-199
ABT-199 is a BH3 mimetic that inhibits Bcl-2 but does not affect Bcl-xl. ABT-199 exhibits anticancer chemotherapeutic activity, inducing Bim-mediated apoptosis in chronic lymphocytic leukemia (CLL) cells. ABT-199 also induces cell death and inhibits tumor growth in acute myelogenous leukemia (AML) models in vitro, ex vivo, and in vivo. ABT-199 is currently under examination as a potential treatment for CLL.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18835003/
| Cas No. |
1257044-40-8 |
|---|---|
| Purity |
≥98% |
| Formula |
C45H50ClN7O7S |
| Formula Wt. |
868.44 |
| IUPAC Name |
4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[3-nitro-4-(oxan-4-ylmethylamino)phenyl]sulfonyl-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide |
| Synonym |
GDC-0199, Venectoclax |
| Solubility |
Soluble in DMSO. |
| Appearance |
Yellow Powder |
Khaw SL, Mérino D, Anderson MA, et al. Both leukaemic and normal peripheral B lymphoid cells are highly sensitive to the selective pharmacological inhibition of prosurvival Bcl-2 with ABT-199. Leukemia. 2014 Jan 9. [Epub ahead of print]. PMID: 24402163.
Pan R, Hogdal LJ, Benito JM, et al. Selective BCL-2 Inhibition by ABT-199 Causes On-Target Cell Death in Acute Myeloid Leukemia. Cancer Discov. 2014 Feb 13. [Epub ahead of print]. PMID: 24346116.
Vandenberg CJ, Cory S. ABT-199, a new Bcl-2-specific BH3 mimetic, has in vivo efficacy against aggressive Myc-driven mouse lymphomas without provoking thrombocytopenia. Blood. 2013 Mar 21;121(12):2285-8. PMID: 23341542.
Souers AJ, Leverson JD, Boghaert ER, et al. ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med. 2013 Feb;19(2):202-8. PMID: 23291630.
