GDC-0152

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Chemical Structure| 873652-48-3 同义名 : -
CAS号 : 873652-48-3
货号 : A852996
分子式 : C25H34N6O3S
纯度 : 99%+
分子量 : 498.64
MDL号 : MFCD26142660
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(100.27 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 45 mg/mL(90.25 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
生物活性
靶点

  • cIAP

    cIAP2-BIR3, Ki:43 nM

    cIAP1-BIR3, Ki:17 nM

  • XIAP

    XIAP-BIR3, Ki:28 nM

    XIAP-BIR2, Ki:112 nM
描述 GDC-0152 disrupts protein−protein interactions involving IAP proteins and pro-apoptotic molecules. In HEK293T cells transiently transfected, GDC-0152 disrupts XIAP binding to partially processed caspase-9 and the association of ML-IAP, cIAP1, and cIAP2 with Smac. In SK-MEL28 melanoma cells, GDC-0152 effectively abolishes the endogenous association of ML-IAP and Smac. It reduces cell viability in MDA-MB-231 breast cancer cells but not in normal human mammary epithelial cells (HMEC). GDC-0152 activates caspases 3 and 7 in a dose- and time-dependent manner. Additionally, GDC-0152 induces rapid degradation of cIAP1 in A2058 melanoma cells, with effective degradation observed at concentrations as low as 10 nM, consistent with its affinity for cIAP1 [1].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
A2058 cells Function assay 15 mins Induction of proteasomal degradation of cIAP1 in human A2058 cells after 15 mins by immunoblotting 22413863
HEK293T cells 1-50 μM Function assay 2 h Inhibition of Flag-tagged XIAP BIR3 domain binding to cIAP1 expressed in human HEK293T cells at 1 to 50 uM after 2 hrs by immunoprecipitation 22413863
MDA-MB-231 cells Cytotoxicity assay 72 h Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescent assay 22413863
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.01mL

0.40mL

0.20mL

10.03mL

2.01mL

1.00mL

20.05mL

4.01mL

2.01mL
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.