Name | PF-9366 |
Synonyms | CS-2703 PF9366 PF-9366 PF 9366 72882-78-1 PF 9366 NEW [1,2,4]Triazolo[4,3-a]quinoline-1-ethanamine, 7-chloro-N,N-dimethyl-5-phenyl- |
CAS | 72882-78-1 |
Molecular Formula | C20H19ClN4 |
Molar Mass | 350.84 |
Density | 1.25±0.1 g/cm3(Predicted) |
Melting Point | 182-183.5 °C(Solv: ethyl acetate (141-78-6); hexane (110-54-3)) |
Solubility | DMSO : 25 mg/mL (71.26 mM; Need ultrasonic) |
Appearance | solid |
Color | Beige |
pKa | 8.75±0.28(Predicted) |
Storage Condition | 2-8°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
In vitro study | PF-9366 is a Mat2A inhibitor with an IC50 of 420 nM and a Kd of 170 nM. PF-9366 there was no substantial off-target activity in GPCR, neural transporters, phosphodiesterases and ion channels. PF-9366 has inhibitory activity against Mat2A in cancer cells. PF-9366 inhibition of cellular S-adenosyl-L-methionine (SAM) in H520 lung cancer cells gave an IC50 of 1.2 μm. PF-9366 was more potent for SAM synthesis in Huh-7 cells with an IC50 of 255 nM and also inhibited cell proliferation with an IC50 of 10 μm. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.85 ml | 14.252 ml | 28.503 ml |
5 mM | 0.57 ml | 2.85 ml | 5.701 ml |
10 mM | 0.285 ml | 1.425 ml | 2.85 ml |
5 mM | 0.057 ml | 0.285 ml | 0.57 ml |
Introduction | PF-9366 is a human metagonine adenosyltransferase 2A (Mat2A) inhibitor with IC50 value of 420 nM, the Kd value was 170 nM. |
in vitro study | PF-9366 is a Mat2A inhibitor with an IC50 of 420 nM and a Kd of 170 nM. PF-9366 there was no substantial off-target activity in GPCR, neural transporters, phosphodiesterases and ion channels. PF-9366 has inhibitory activity against Mat2A in cancer cells. PF-9366 inhibition of cellular S-adenosyl-L-methionine (SAM) in H520 lung cancer cells gave an IC50 of 1.2 μm. PF-9366 was more potent for SAM synthesis in Huh-7 cells with an IC50 of 255 nM and also inhibited cell proliferation with an IC50 of 10 μm. |
biological activity | PF-9366 is a human metagonine adenosyltransferase 2A (Mat2A) inhibitor with IC50 value of 420 nM, the Kd value was 170 nM. |
Target | TargetValue hMat2A (Cell-free assay) 170 nM(Kd) hMat2A (Cell-free assay) 420 nM |
Target | Value |
hMat2A (Cell-free assay) | 170 nM(Kd) 420 nM |