2750570-55-7
2750570-55-7 structure
- Name: BI-0474
- Chemical Name: BI-0474
- CAS Number: 2750570-55-7
- Molecular Formula: C30H37N9O2S
- Molecular Weight: 587.74
- Catalog: Signaling Pathways GPCR/G Protein Ras
- Create Date: 2022-11-16 14:21:58
- Modify Date: 2024-01-03 20:22:54
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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[1].
| Name | BI-0474 |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| Target |
KRASG12C[1]. |
| 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 EC50 of 26 nM. |
| 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. |
| References |
| Molecular Formula | C30H37N9O2S |
|---|---|
| Molecular Weight | 587.74 |