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BLU-945

Cat. No. M11448
BLU-945  Structure
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Biological Activity

Blu-945 is a potent inhibitor of selective epidermal growth factor receptor (EGFR). EGFR is a member of the erbB receptor family, which includes receptors for transmembrane protein tyrosine kinases. Blu-945 effectively inhibits EGFR with L858R and/or exon 19 deletion mutations, T790M mutations and C797S mutations. Blu-945 contributes to effective administration and reduces egFR-mediated targeted toxicity. Blu-945 has the potential to study cancer diseases (information extracted from patent WO2021133809A1, compound 112).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 556.7
Formula C28H37FN6O3S
CAS Number 2660250-10-0
Purity
Solubility N/A
Storage at -20°C
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