Alvocidib Prodrug TP-1287 is an orally bioavailable, highly soluble phosphate prodrug of alvocidib, a potent inhibitor of cyclin-dependent kinase-9 (CDK9), with potential antineoplastic activity. Upon administration of the phosphate prodrug TP-1287, the prodrug is enzymatically cleaved at the tumor site and the active moiety alvocidib is released. Alvocidib targets and binds to CDK9, thereby reducing the expression of CDK9 target genes such as the anti-apoptotic protein MCL-1, and inducing G1 cell cycle arrest and apoptosis in CDK9-overexpressing cancer cells.
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名称 | TP1287 |
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Iupac 化学名称 | 2-(2-chlorophenyl)-5-hydroxy-8-((3S,4R)-3-hydroxy-1-methylpiperidin-4-yl)-4-oxo-4H-chromen-7-yl dihydrogen phosphate |
同义词 | TP-1287 ; Alvocidib Phosphate ; Alvocidib Prodrug TP-1287 ; TP1287 ; TP 1287 ; |
英文同义词 | TP-1287 ; Alvocidib Phosphate ; Alvocidib Prodrug TP-1287 ; TP1287 ; TP 1287 ; |
分子式 | C21H21ClNO8P |
分子量 | 481.82 |
Smile | OC1=C2C(OC(C3=C(Cl)C=CC=C3)=CC2=O)=C([C@@H]4[C@H](O)CN(C)CC4)C(OP(O)(O)=O)=C1 |
InChiKey | YRNFLVUMZIRYKY-BLLLJJGKSA-N |
InChi | InChI=1S/C21H21ClNO8P/c1-23-7-6-12(16(26)10-23)19-18(31-32(27,28)29)9-15(25)20-14(24)8-17(30-21(19)20)11-4-2-3-5-13(11)22/h2-5,8-9,12,16,25-26H,6-7,10H2,1H3,(H2,27,28,29)/t12-,16+/m0/s1 |
Cas号 | 2044686-42-0 |
相关CAS号 | 2044686-42-0 |
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