| Identification | Back Directory | [Name]
GDC-0152 | [CAS]
873652-48-3 | [Synonyms]
CS-2247
GDC-0152
GDC0152;GDC 0152.
GDC-0152 USP/EP/BP
GDC-0152; GDC0152; GDC 0152.
L-Prolinamide, N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-N-(4-phenyl-1,2,3-thiadiazol-5-yl)-
(S)-1-((S)-2-Cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)-N-(4-phenyl-1,2,3-thiadiazol-5-yl)pyrrolidine-2-carboxamide | [Molecular Formula]
C25H34N6O3S | [MDL Number]
MFCD26142660 | [MOL File]
873652-48-3.mol | [Molecular Weight]
498.64 |
| Hazard Information | Back Directory | [Uses]
GDC 0152 is a peptidomimetic small molecule antagonist of inhibitor of apoptosis (IAP) proteins with antitumor activity. | [Biological Activity]
gdc-0152 is a potent small-molecule antagonist of inhibitor of apoptosis (iap) proteins, including ml-iap, xiap, ciap1 and ciap2, that binds to the bir domain of ml-iap and the bir3 domains of xiap, ciap1 and ciap2 with values of inhibition constant ki of 14 nm, 28 nm, 17 nm and 43 nm respectively. gdc-0152 potentially inhibits tumor growth of breast cancer by promoting ciap1 degradation and inducing caspase-3/7 activation which result in the decreasing of cell viability of breast cancer cells with normal epithelial cells unaffected. in recent studies, gdc-0152 shows its ability to disrupt the binding of xiap to caspase-9 and the association of ml-iap, ciap1 and ciap2 with smac in hek293t cells.flygare ja, beresini m, budha n, chan h, chan it, cheeti s, cohen f, deshayes k, doerner k, eckhardt sg, elliott lo, feng b, franklin mc, reisner sf, gazzard l, halladay j, hymowitz sg, la h, lorusso p, maurer b, murray l, plise e, quan c, stephan jp, young sg, tom j, tsui v, um j, varfolomeev e, vucic d, wagner aj, wallweber hj, wang l, ware j, wen z, wong h, wong jm, wong m, wong s, yu r, zobel k, fairbrother wj. discovery of a potent small-molecule antagonist of inhibitor of apoptosis (iap) proteins and clinical candidate for the treatment of cancer (gdc-0152). j med chem. 2012;55(9):4101-4113 | [target]
XIAP | [storage]
Store at -20°C |
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