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BI-0474

Cat. No. M21533
BI-0474 Structure
Size Price Availability Quantity
5mg USD 990  USD990 In stock
10mg USD 1350  USD1350 In stock
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Quality Control & Documentation
Biological Activity

BI-0474 is a covalent KRASG12C inhibitor. The IC50 value for GDP-KRAS::SOS1 protein-protein interaction was 7.0 nM. BI-0474 also showed better antitumor activity in non-small cell lung cancer xenograft models.

Chemical Information
Molecular Weight 587.74
Formula C30H37N9O2S
CAS Number 2750570-55-7
Solubility (25°C) N/A
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Joachim Brker, et al. J Med Chem. Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor

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  Catalog
Abmole Inhibitor Catalog




Keywords: BI-0474 supplier, Ras, inhibitors, activators


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