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.
| Molecular Weight | 350.84 |
| Formula | C20H19ClN4 |
| CAS Number | 72882-78-1 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
| Related Adenosyltransferase Products |
|---|
| MAT2A-IN-10
MAT2A-IN-10 is an orally active MAT2A inhibitor with an IC50 of 26 nM. |
| MAT2A-IN-12
MAT2A Allosteric inhibitor 2 is a potent and selective MAT2A allosteric inhibitor with an IC50 of 5 nM. |
| MAT2A inhibitor 3
MAT2A inhibitor 3 is a methionine adenosyltransferase 2A (MAT2A) inhibitor, with an IC50 of <200 nM. MAT2A inhibitor 3 can be used for the research of cancers. |
| MAT2A inhibitor 2
MAT2A inhibitor 2 is a methionine adenosyltransferase 2A (MAT2A) inhibitor. |
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