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CH7233163

Cat. No. M40642
CH7233163 Structure
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Biological Activity

CH7233163 is a non-covalent ATP-competitive EGFR- del19 /T790M/C797S inhibitor that can achieve potent inhibitory activity and mutation selection by exploiting multiple interactions with the αC helix conformation of EGFR, with antitumor activity, and can be used in studies related to non-small cell lung cancer (NSCLC).

Chemical Information
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] Ravi Saini et al. Sci Rep. Discovery of the allosteric inhibitor from actinomyces metabolites to target EGFRCSTMLR mutant protein: molecular modeling and free energy approach

[2] Kenji Kashima et al. Mol Cancer Ther. CH7233163 Overcomes Osimertinib-Resistant EGFR-Del19/T790M/C797S Mutation

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Keywords: CH7233163 supplier, EGFR/HER2, inhibitors, activators


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