GDC-0152

Inhibitor of apoptosis proteins (IAPs), which block various signaling pathways leading to apoptotic cell death, are commonly over-expressed in cancer cells. GDC-0152 is a potent inhibitor of specific IAPs that binds baculoviral IAP repeat (BIR) domains (Kis = 28, 14, 17, and 43 nM for XIAP BIR3, NL-IAP BIR, BIRC2 (c-IAP1) BIR3, and BIRC3 (c-IAP2) BIR3, respectively). GDC-0152 induces activation of caspases, decreasing the viability of cancer cells without affecting normal cells. It is orally bioavailable and suppresses tumor growth in breast cancer xenografts in mice. GDC-0152 also induces NF-kappaB transcriptional activity, resulting in the expression of several cytokines, including TNF-alpha. In dogs and rats, but not humans, this leads to a pronounced inflammatory response.Formal Name: N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-N-(4-phenyl-1,2,3-thiadiazol-5-yl)-L-prolinamide. CAS Number: 873652-48-3. Molecular Formula: C25H34N6O3S. Formula Weight: 498.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 10 mg/ml, Ethanol: 10 mg/ml. lambdamax: 230, 255, 293 nm. SMILES: O=C(N[C@@H](C1CCCCC1)C(N2CCC[C@H]2C(NC3=C(C4=CC=CC=C4)N=NS3)=O)=O)[C@@H](NC)C. InChi Code: InChI=1S/C25H34N6O3S/c1-16(26-2)22(32)27-21(18-12-7-4-8-13-18)25(34)31-15-9-14-19(31)23(33)28-24-20(29-30-35-24)17-10-5-3-6-11-17/h3,5-6,10-11,16,18-19,21,26H,4,7-9,12-15H2,1-2H3,(H,27,32)(H,28,33)/t16-,19-,21-/m0/s1. InChi Key: WZRFLSDVFPIXOV-LRQRDZAKSA-N.