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名称: AT-101英文名称: AT-101产品编号 A127496
CAS号: 90141-22-3分子式 C30H30O8分子量518.55
溶解性 | DMSO >80 mg/ml Ethanol >80 mg/ml |
存贮条件 | 储存温度-20°C |
生化机理 |
AT-101 is orally bioavailable solvate of R-(-)-enantiomer of gossypol with potential antineoplastic activity. As a BH3 mimetic, AT-101 binds to the hydrophobic surface binding groove BH3 of the anti-apoptotic proteins Bcl-2 and Bcl-xL, blocking their heterodimerization with pro-apoptotic members of the Bcl-2 family of proteins such as Bad, Bid, and Bim; this may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. AT-101 induces apoptosis in vitro through activation of caspase-9; cytotoxic to multiple myeloma and drug-resistant cell lines. AT-101 delays onset of androgen-independent growth of VCaP prostate cancer xenografts in vivo. |
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