ABT-737 is a selective and potent small molecule inhibitor of protein Bcl-2, Bcl-XL, and Bcl-w. Like a BAD BH3 peptide, ABT-737 binds to and antagonizes anti-apototic Bcl-2 family proteins instead of directly activating the apoptotic process. ABT-737 binds with high affinity (ki < 1nm) to Bcl-XL, Bcl-2 and Bcl-w, but not to Bcl-B, Mcl-1 and Al protein.
ABT-737 displays a wide range of single-agent activity against cells from lymphoma, leukemia, solid tumor SCLC, and primary cells derived from patient. In animal models, ABT-737 causes tumor regression and improves survival1-2. ABT-737 has shown synergistic anti-tumor activity when used together with vorinostat or bemicitabine3,4.
Technical information:
| Chemical Formula: | C42H45CIN6O5S2 | |
| CAS #: | 852808-04-9 | |
| Molecular Weight: | 813.43 | |
| Purity: | >98% | |
| Apperance: | Off white solid | |
| Chemical Name: | 4-[4-[(4'-Chloro[1,1'-biphenyl]-2-yl)methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(dimethylamino) -1-[(phenylthio)methyl]propyl]amino]-3-nitrophenyl]sulfonyl]benzamide | |
| Solubility: | Up to 50 mM in DMSO |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Oltersdorf, T. et al. An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature. 2005 Jun 2;435(7042):677-81. |
| 2. | Van Deelft , MF. et al. The BH3 mimetic ABT-737 targets selective Bcl-2 proteins and efficiently induces apoptosis via Bak/Bax if Mcl-1 is neutralized. Cancer Cell. 2006 Nov;10(5):389-99. |
| 3. | Zhang, C. et al. Synergistic anti-tumor activity of gemcitabine and ABT-737 in vitro and in vivo through disrupting the interaction of USP9X and Mcl-1. Mol Cancer Ther. 2011 Jul;10(7):1264-75. |
| 4. | Wiegmans AP, et al. Deciphering the molecular events necessary for synergistic tumor cell apoptosis mediated by the histone deacetylase inhibitor vorinostat and the BH3 mimetic ABT-737. Cancer Res. 2011 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
