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BI-0474

CAS No. 2750570-55-7

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
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Kras
  • Research Area
    ——
  • Indication
    ——

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
    ——

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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