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抑制剂描述:

产品名称:GDC-0152

产品别名:见爱必信官网

英文别名:GDC-0152

靶点:IAP

CAS:873652-48-3

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

GDC-0152 is a potent inhibitor of IAPs; binds to the XIAP BIR3 domain, the BIR domain of ML-IAP, and the BIR3 domains of cIAP1 and cIAP2 with K(i) values of 28, 14, 17, and 43 nM, respectively.

溶解性:10 mM in DMSO

体外研究:

GDC-0152 can block protein?protein interactions that involve IAP proteins and pro-apoptotic molecules. Using transiently transfected HEK293T cells, GDC-0152 is shown to disrupt XIAP binding to partially processed caspase-9 and to disrupt the association of ML-IAP, cIAP1, and cIAP2 with Smac. In melanoma SK-MEL28 cells, the endogenous association of ML-IAP and Smac is effectively also abolished by GDC-0152. GDC-0152 lead to a decrease in cell viability in the MDA-MB-231 breast cancer cell line, while having no effect on normal human mammary epithelial cells (HMEC). GDC-0152 is found to activate caspases 3 and 7 in a dose- and time-dependent manner. GDC-0152 is shown to induce rapid degradation of cIAP1 in A2058 melanoma cells. It effectively induces degradation of cIAP1 at concentrations as low as 10 nM, consistent with its affinity for cIAP1.

体内研究: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.

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