PKI-587 is a potent inhibitor to PI3K-, PI3K-, and mTOR (FRAP) with IC50 of 0.4 nM, 5.4 nM, and 1.6 nM, respectively. PKI-587 also exhibits potency against the most frequently occurring mutant forms of PI3K, notably the H1047R and E545K with IC50 of 0.6 nM and 0.6 nM, respectively. PF-05212384 inhibitory actions against PI3Ks and mTORs causes tumor cell growth inhibition in MDA-361 and PC3-MM2 cell lines with IC50 of 4 nM and 13.1 nM, respectively.
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名称 | PKI-587 |
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Iupac 化学名称 | 1-(4-(4-(dimethylamino)piperidine-1-carbonyl)phenyl)-3-(4-(4,6-dimorpholino-1,3,5-triazin-2-yl)phenyl)urea |
同义词 | PF-05212384; PF5212384; PF05212384; PF 05212384; Gedatolisib |
英文同义词 | PF-05212384; PF5212384; PF05212384; PF 05212384; Gedatolisib |
分子式 | C32H41N9O4 |
分子量 | 615.73 |
Smile | CN(C1CCN(CC1)C(=O)C1=CC=C(C=C1)NC(=O)NC1=CC=C(C=C1)C1=NC(=NC(=N1)N1CCOCC1)N1CCOCC1)C |
InChiKey | DWZAEMINVBZMHQ-UHFFFAOYSA-N |
InChi | InChI=1S/C32H41N9O4/c1-38(2)27-11-13-39(14-12-27)29(42)24-5-9-26(10-6-24)34-32(43)33-25-7-3-23(4-8-25)28-35-30(40-15-19-44-20-16-40)37-31(36-28)41-17-21-45-22-18-41/h3-10,27H,11-22H2,1-2H3,(H2,33,34,43) |
Cas号 | 1197160-78-3 |
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