|(S)-1-((S)-2-环己基-2-((S)-2-(甲基氨基)丙酰胺基)乙酰基)-N-(4-苯基-1,2,3-噻二唑-5-基)吡咯烷-2-甲酰胺|CsnPharm

CAS No.: 873652-48-3

GDC-0152 Catalog No. CSN18513

Synonyms: RG-7419

GDC-0152 is a potent inhibitor of IAPs and 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.

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实验方案

技术信息

生物活性

描述GDC-0152 is a potent inhibitor of IAPs and 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.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

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临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00977067	Solid Cancers	Phase 1	Terminated(The study was termi... more >>nated early by the Sponsor for reasons unrelated to patient safety or anti-tumor activity.) Collapse <<	-	-

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0055 mL
- 10.0273 mL
- 20.0545 mL
- 5 mM
- 0.4011 mL
- 2.0055 mL
- 4.0109 mL
- 10 mM
- 0.2005 mL
- 1.0027 mL
- 2.0055 mL

技术信息

CAS号

873652-48-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H34N6O3S

运输

蓝冰

分子量

498.64

别名

RG-7419

溶解度

DMSO	150.0 mg/mL (300.8 mM)
Water	125.0 mg/mL (250.7 mM)

动物实验配方

30% propylene glycol+5% Tween 80+65% water

5 mg/mL

suspension

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