GDC-0152

Research use only, not for human use.

GDC-0152 is a potent antagonist of XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 28 nM, 14 nM, 17 nM and 43 nM, respectively.

GDC-0152 is a potent antagonist of XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 28 nM, 14 nM, 17 nM and 43 nM, respectively; less affinity shown to cIAP1-BIR2 and cIAP2-BIR2. Phase 1. (In Vivo):GDC-0152 has moderate predicted hepatic clearance based on metabolic stability assays conducted using human liver microsomes. Plasma?protein binding of GDC-0152 is moderate and comparable among mice (88?91%), rats (89?91%), dogs (81?90%), monkeys (76?85%), and humans (75?83%) over the range of concentrations investigated (0.1?100 μM); higher plasma?protein binding is observed in rabbits (95?96%). GDC-0152 does not preferentially distribute to red blood cells with blood?plasma partition ratios ranging from 0.6 to 1.1 in all species tested. The pharmacokinetics for GDC-0152 is achieved with a C max of 53.7 μM and AUC of 203.5 h·μM.

——

——

——

Apoptosis

IAP

cIAP1-BIR3| cIAP2-BIR3| MLXBIR3SG| XIAP-BIR2| XIAP-BIR3

Cancer

——

873652-48-3

498.64

C25H34N6O3S

>98% (HPLC)

DMSO:99 mg/mL (198.54 mM); Ethanol:99 mg/mL (198.54 mM); Water:3 mg/mL (6.01 mM)

CN[C@@H](C)C(=O)N[C@@H](C1CCCCC1)C(=O)N1CCC[C@H]1C(=O)NC1=C(N=NS1)C1=CC=CC=C1 |r,c:28,34,36,t:26,32|

——

(-20℃)

With Ice Pack

≥ 2 years