ABT-263
ABT-263 is a BH3 mimetic that inhibits Bcl-2, Bcl-ω, and Bcl-xl. ABT-263’s inhibition of Bcl-xl results in thrombocytopenia by inducing apoptotic death of platelets, limiting its usage. ABT-263 exhibits anticancer chemotherapeutic activity and shows some benefit in clinical trials. In chronic lymphocytic leukemia (CLL) cells, ABT-263 inhibits cell proliferation. In cellular and animal models of cancers with solid tumors, ABT-263 enhances the chemotherapeutic activity of several co-administered treatments.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18835033
| Cas No. |
923564-51-6 |
|---|---|
| Purity |
≥98% |
| Formula |
C47H55ClF3N5O6S3 |
| Formula Wt. |
974.61 |
| IUPAC Name |
4-[4-[[2-(4-chlorophenyl)-5,5-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide |
| Synonym |
Navitoclax, A-855071 |
| Appearance |
White to off white powder |
Debrincat MA, Pleines I, Lebois M, et al. BCL-2 is dispensable for thrombopoiesis and platelet survival. Cell Death Dis. 2015 Apr 16;6:e1721. PMID: 25880088.
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.
Balakrishnan K, Gandhi V. Bcl-2 antagonists: a proof of concept for CLL therapy. Invest New Drugs. 2013 Oct;31(5):1384-94. PMID: 23907405.
Rudin CM, Hann CL, Garon EB, et al. Phase II study of single-agent navitoclax (ABT-263) and biomarker correlates in patients with relapsed small cell lung cancer. Clin Cancer Res. 2012 Jun 1;18(11):3163-9. PMID: 22496272.
Chen J, Jin S, Abraham V, et al. The Bcl-2/Bcl-X(L)/Bcl-w inhibitor, navitoclax, enhances the activity of chemotherapeutic agents in vitro and in vivo. Mol Cancer Ther. 2011 Dec;10(12):2340-9. PMID: 21914853.
