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PF-07284892

Cat. No. M31081
PF-07284892 Structure
Synonym:

ARRY-558

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Quality Control & Documentation
Biological Activity

PF-07284892 (ARRY-558) is a potent and orally activity SHP2 inhibitor with an IC50 value of 21 nM. PF-07284892 decreases theexpression of pERK.

Chemical Information
Molecular Weight 438.98
Formula C22H23ClN6S
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Alexander Drilon, et al. Cancer Discov. SHP2 Inhibition Sensitizes Diverse Oncogene-Addicted Solid Tumors to Re-treatment with Targeted Therapy

[2] Alberto Hernando-Calvo, et al. Cancer Discov. Patient-Centric Approaches for Phase I Combination Trials Come on Stage

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  Catalog
Abmole Inhibitor Catalog




Keywords: PF-07284892, ARRY-558 supplier, Phosphatase, inhibitors, activators


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