PF-9366 is a novel inhibitor of human methionine adenosyltransferase 2A (Mat2A), with IC50 of 420 nM and Kd of 170 nM. PF-9366 inhibits cellular S-Adenosyl-L-methionine (SAM) production with an IC50 of 1.2 μM in H520 lung carcinoma cells. PF-9366 is more potent in Huh-7 cells against SAM synthesis, with an IC50 of 255 nM, and also suppresses the proliferation of cells with an IC50 of 10 μM.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥ 20 mg/mL|
Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A
Casey L Quinlan, et al. Nat Chem Biol. 2017 Jul;13(7):785-792. PMID: 28553945.
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