BI-0474

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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。

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KRAS^G12C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 potentKRAS^G12Cinhibitor 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.