BI-0474 Chemical Properties

Boiling point:

879.4±75.0 °C(Predicted)

Density 

1.38±0.1 g/cm3(Predicted)

pka

7.13±0.70(Predicted)

form 

Solid

color 

White to off-white

InChIKey

CKAMBYUZKWQCKJ-ADSBAMQRSA-N

SMILES

C12CCC[C@@](C3ON=C(C4=NC(N5CCN(C)C[C@@H]5C)=CC(N5CCN(C(=O)C=C)CC5)=C4)N=3)(C)C=1C(C#N)=C(N)S2

BI-0474 Usage And Synthesis

Description

BI-0474 is a potent KRASG12C inhibitor with an IC50 value of 7.0 nM.

Uses

BI-0474 is a potent KRAS^G12C inhibitor with an IC₅₀ value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. It 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.

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