BI-0474( —— )

Catalog No. M36283 CAS No. 2750570-55-7

BI-0474 is a potent KRASG12C inhibitor that inhibits GDP-KRAS::SOS1 protein-protein interactions with an IC50 value of 7.0 nM.BI-0474 exhibits significant antiproliferative activity against NCI-H358 cells harboring the G12C mutation, and shows significant anti-tumor activity in a non-small cell lung cancer xenograft model.

Purity : >98% (HPLC)

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Biological Information

Product Name

BI-0474
Note

Research use only, not for human use.
Brief Description

BI-0474 is a potent KRASG12C inhibitor that inhibits GDP-KRAS::SOS1 protein-protein interactions with an IC50 value of 7.0 nM.BI-0474 exhibits significant antiproliferative activity against NCI-H358 cells harboring the G12C mutation, and shows significant anti-tumor activity in a non-small cell lung cancer xenograft model.
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.
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.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.
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.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.
Synonyms

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Pathway

Others
Target

Other Targets
Recptor

Kras
Research Area

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Indication

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Chemical Information

CAS Number

2750570-55-7
Formula Weight

587.74
Molecular Formula

C30H37N9O2S
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 100 mg/mL (170.14 mM; Ultrasonic )
SMILES

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
Chemical Name

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Shipping & Storage Information

Storage

(-20℃)
Shipping

With Ice Pack
Stability

≥ 2 years

Reference

1. Br?ker J, et al. Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor. J Med Chem. 2022 Oct 27. ?

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