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BI-0474

Catalog No. T69529   CAS 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. activity.BI-0474 can be used for cancer research.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
BI-0474 Chemical Structure
BI-0474, CAS 2750570-55-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 432.00
5 mg In stock $ 987.00
10 mg In stock $ 1,370.00
25 mg In stock $ 1,980.00
50 mg In stock $ 2,730.00
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Purity: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
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. activity.BI-0474 can be used for cancer research.
Targets&IC50 KRAS-SOS1:7 nM
In vitro BI-0474 (1-10,000 nM; 3 days; NCI-H358 cells carrying a G12C mutation) inhibited proliferation of NCI-H358 cells with an EC50 of 26 nM.[1]
In vivo BI-0474 (40 mg/kg; i.p.; single daily for 3 days; NMRI nude mice) shows anti-tumor efficacy and pharmacodynamic biomarker modulation. This led to the induction of programmed cell death in this xenograft model.[1]
Molecular Weight 587.74
Formula C30H37N9O2S
CAS No. 2750570-55-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Kinase Inhibitor Library Membrane Protein-targeted Compound Library Inhibitor Library GPCR Compound Library Bioactive Compounds Library Max Bioactive Compound Library

Related Products

Related compounds with same targets
KRAS inhibitor-8 BQU57 (Rac)-Antineoplaston A10 Kras4B G12D-IN-1 KRas G12C inhibitor 2 Pan-RAS-IN-1 Rhosin hydrochloride MRTX-1257

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Keywords

BI-0474 2750570-55-7 GPCR/G Protein MAPK Ras inhibitor inhibit

 

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