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BI-0474
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。
BI-0474图片
CAS NO:2750570-55-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
BI-0474 是一种强效的KRASG12C抑制剂,其对GDP-KRAS::SOS1蛋白-蛋白相互作用的IC50值为 7.0 nM。BI-0474 对携带G12C突变的 NCI-H358 细胞具有较好的抗增殖活性。BI-0474 还在非小细胞肺癌异种移植模型中显示出较好的抗肿瘤活性。
生物活性

BI-0474 is a potentKRASG12Cinhibitor with anIC50value of 7.0 nM for theGDP-KRAS::SOS1protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying theG12Cmutation. BI-0474 also shows good anti-tumour activity in non-small cell lungcancerxenograft models[1].

IC50& Target

KRAS-SOS1

7.0 nM (IC50)

体外研究
(In Vitro)

BI-0474 (1-10,000 nM; 3 days) shows potent antiproliferative activity of 26 nM on NCI-H358 cells carrying a G12C mutation[1].

Cell Proliferation Assay[1]

Cell Line:NCI-H358 cells (carrying a G12C mutation)
Concentration:1-10,000 nM
Incubation Time:3 days
Result:Inhibited proliferation of NCI-H358 cells with an EC50of 26 nM.
体内研究
(In Vivo)

BI-0474 (40 mg/kg; i.p.; single daily for 3 days) shows anti-tumor efficacy and pharmacodynamic biomarker modulation in an NCI-H358 cell line-derived non-small cell lung cancer xenograft model[1].

Animal Model:NMRI nude mice (NCI-H358 cell line-derived non-small cell lung cancer xenograft model)[1].
Dosage:40 mg/kg
Administration:Intraperitoneal administration; single daily for 3 days
Result:Led to induction of programmed cell death in this xenograft model.
分子量

587.74

Formula

C30H37N9O2S

CAS 号

2750570-55-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.