BI-0474

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

BI-0474 is a potent KRASG12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models.

BI-0474 (1-10,000 nM; 3 days) shows potent antiproliferative activity of 26 nM on NCI-H358 cells carrying a G12C mutation.Cell Proliferation Assay 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 EC50 of 26 nM.

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

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Others

Other Targets

Kras

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2750570-55-7

587.74

C30H37N9O2S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (170.14 mM; 超声助溶 )

C[C@]1(C2=C(SC(N)=C2C#N)CCC1)C3=NC(=NO3)C=4N=C(C=C(C4)N5CCN(C(C=C)=O)CC5)N6[C@@H](C)CN(C)CC6

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(-20℃)

With Ice Pack

≥ 2 years