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GDC-0152(RG7419)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GDC-0152(RG7419)图片
CAS NO:873652-48-3
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)498.64
FormulaC25H34N6O3S
CAS No.873652-48-3
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 99 mg/mL (198.5 mM)
Water: 3 mg/mL (6.0 mM)
Ethanol: 99 mg/mL (198.5 mM)
Solubility (In vivo)30% Propylene glycol, 5% Tween 80, 65% D5W: 5mg/mL
Synonym/Chemical NameGDC0152; RG-7419; GDC0152; RG 7419; GDC 0152; RG7419.; (2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-(4-phenylthiadiazol-5-yl)pyrrolidine-2-carboxamide
实验参考方法
In VitroGDC-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 VivoGDC-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%).
Animal modelHuman-tumor xenograft mouse models of MDA-MB-231 breast cancer
Formulation & Dosagephosphate-buffered saline; 10, 50, 100 mg/kg; Oral
References[1] Flygare JA, et al. J Med Chem, 2012, 55(9), 4101-4113.
生物活性




Flygare JA, et al. J Med Chem, 2012, 55(9), 4101-4113.