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SynKinase
ABT-737
Product Details | |
---|---|
Synonyms | ABT737 |
Product Type | Chemical |
Properties | |
Formula |
C42H45ClN6O5S2 |
MW | 813.4 |
CAS | 852808-04-9 |
Purity Chemicals | ≥95% |
Appearance | Solid. |
Solubility | Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol. |
Declaration | Manufactured by SynKinase. |
Other Product Data |
Target: Bcl-2 | Kinase Group: PPI | Substrate: N/A Click here for Original Manufacturer Product Datasheet Our product description may differ slightly from the original manufacturers product datasheet. |
InChi Key | HPLNQCPCUACXLM-PGUFJCEWSA-N |
Shipping and Handling | |
Shipping | AMBIENT |
Short Term Storage | +4°C |
Long Term Storage | -20°C |
Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
Documents | |
MSDS | Download PDF |
Product Specification Sheet | |
Datasheet | Download PDF |
ABT-737 is a small-molecule inhibitor of the anti-apoptotic proteins Bcl-2, Bcl-X(L) and Bcl-w, with an affinity two to three orders of magnitude more potent than previously reported compounds. Mechanistic studies reveal that ABT-737 does not directly initiate the apoptotic process, but enhances the effects of death signals, displaying synergistic cytotoxicity with chemotherapeutics and radiation. ABT-737 exhibits single-agent-mechanism-based killing of cells from lymphoma and small-cell lung carcinoma lines, as well as primary patient-derived cells, and in animal models, ABT-737 improves survival, causes regression of established tumors, and produces cures in a high percentage of the mice. ABT-737 binds to Bcl-2, Bcl-xL and Bcl-w with very high affinities (Ki <1 nM) and also shows a very high specificity over Mcl-1 and A1.
- An inhibitor of Bcl-2 family proteins induces regression of solid tumours: T. Oltersdorf, et al.; Nature 435, 677 (2005)
- Synthesis and biological activities of new di- and trimeric quinoline derivatives: S. Broch, et al.; Bioorg. Med. Chem. 18, 7132 (2010)
- Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL: B.E. Sleebs, et al.; J. Med. Chem. 56, 5514 (2013)