BI-0474

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].

Product Specifications

CAS Number

[2750570-55-7]

UNSPSC

12352005

Target

Ras; SOS1

Type

Reference compound

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bi-0474.html

Purity

99.83

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

N#CC1=C(N)SC2=C1[C@@](C)(C3=NC(C4=NC(N5[C@@H](C)CN(C)CC5)=CC(N6CCN(C(C=C)=O)CC6)=C4)=NO3)CCC2

Molecular Formula

C30H37N9O2S

Molecular Weight

587.74

References & Citations

[1]Bröker 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.