货号	规格	价格	上海	北京	武汉	南京
S81047-5mg	≥98%	￥560.00 S81047-5mg ￥560.00 现货	10 10	-	-	-
S81047-10mg	≥98%	￥900.00 S81047-10mg ￥900.00 现货	10 10	-	-	-
S81047-25mg	≥98%	￥1250.00 S81047-25mg ￥1250.00 现货	8 8	-	-	-
S81047-50mg	≥98%	￥2000.00 S81047-50mg ￥2000.00 现货	8 8	-	-	-
S81047-100mg	≥98%	￥3200.00 S81047-100mg ￥3200.00 现货	5 5	-	-	-

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产品描述：

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

靶点：

Ki: 28 nM (XIAP BIR3), 14 nM (MLIAP-BIR3), 17 nM (cIAP1-BIR3), 43 nM (cIAP2-BIR3);IAP

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

参考文献：

1. Flygare JA, et al. 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 May 10;55(9):4101-13.

溶解性：

Soluble in DMSO、Ethanol

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.005 ml	10.027 ml	20.055 ml
5 mM	0.401 ml	2.005 ml	4.011 ml
10 mM	0.201 ml	1.003 ml	2.005 ml
50 mM	0.04 ml	0.201 ml	0.401 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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