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GDC-0152

GDC-0152

产品编号 T6299   CAS 873652-48-3
别名: GDC0152

GDC-0152 是一种 IAP 抑制剂,可以与 XIAP、cIAP1和cIAP2的 BIR3 结合域,以及ML-IAP 的 BIR 结合域结合,Ki 值分别为 28 nM、17 nM、43 nM 和 14 nM。

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GDC-0152 Chemical Structure
GDC-0152, CAS 873652-48-3
规格 价格/CNY 货期 数量
1 mg ¥ 327 现货
2 mg ¥ 468 现货
5 mg ¥ 775 现货
10 mg ¥ 1,230 现货
25 mg ¥ 2,260 待询
50 mg ¥ 3,730 待询
1 mL * 10 mM (in DMSO) ¥ 678 现货
产品目录号及名称: GDC-0152 (T6299)
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纯度: 99.32%
纯度: 98.23%
纯度: 97.18%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 GDC-0152 is a potent inhibitor of IAPs.
靶点活性 cIAP1-BIR3:17 nM(Ki), MLXBIR3SG:14 nM(Ki), XIAP-BIR3:28 nM(Ki), XIAP-BIR2:112 nM(Ki), cIAP2-BIR3:43 nM(Ki)
体外活性 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. The endogenous association of ML-IAP and Smac is effectively also abolished by GDC-0152 in melanoma SK-MEL28 cells. 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.
体内活性 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 of 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. [1]
激酶实验 Fluorescence polarization-based competition assay: Inhibition constants ( Ki ) for the antagonists are determined by addition of the IAP protein constructs to wells containing serial dilutions of the antagonists or the peptide AVPW, and the Hid-FAM probe or AVP-diPhe-FAM probe, as appropriate, in the polarization buffer. Samples are read after a 30-minute incubation. Fluorescence polarization values are plotted as a function of the antagonist concentration, and the IC50 values are obtained by fitting the data to a 4-parameter equation using software. Ki values for the antagonists are determined from the IC50 valued.
细胞实验 MDA-MB-231 breast carcinoma cells and HMECs are treated with the indicated concentrations of GDC-0152. Cell death is assessed using the CellTiter-Glo luminescent cell viability assay 72 h following the start of treatment.(Only for Reference)
别名 GDC0152
分子量 498.64
分子式 C25H34N6O3S
CAS No. 873652-48-3

存储

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 92 mg/mL (184.5 mM)

Ethanol: 92 mg/mL (184.5 mM)

H2O: 3 mg/mL (6.01 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol / H2O 1 mM 2.0055 mL 10.0273 mL 20.0545 mL 50.1364 mL
5 mM 0.4011 mL 2.0055 mL 4.0109 mL 10.0273 mL
DMSO / Ethanol 10 mM 0.2005 mL 1.0027 mL 2.0055 mL 5.0136 mL
20 mM 0.1003 mL 0.5014 mL 1.0027 mL 2.5068 mL
50 mM 0.0401 mL 0.2005 mL 0.4011 mL 1.0027 mL
100 mM 0.0201 mL 0.1003 mL 0.2005 mL 0.5014 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Flygare JA, et al. J Med Chem, 2012, 55(9), 4101-4113.
Polygalacin D Xevinapant BV6 LCL161 Embelin AZD5582 AZD5582 TFA SM-164

相关化合物库

该产品包含在如下化合物库中:
铜死亡化合物库 NO PAINS 化合物库 细胞凋亡化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

GDC-0152 873652-48-3 Apoptosis IAP Inhibitor inhibit GDC0152 GDC 0152 inhibitor

 

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