Pyrido[2,3-d]pyrimidin-7(8H)-one, 2-amino-8-cyclopentyl-4-methyl-6-(1H-pyrazol-4-yl)- Chemical Properties

Boiling point:

637.3±65.0 °C(Predicted)

Density 

1.422±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

Soluble in DMSO

form 

Solid

pka

13.59±0.50(Predicted)

color 

Off-white to light yellow

Pyrido[2,3-d]pyrimidin-7(8H)-one, 2-amino-8-cyclopentyl-4-methyl-6-(1H-pyrazol-4-yl)- Usage And Synthesis

Uses

PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.

in vivo

IC 50

PI3Kα: 7 nM (IC₅₀, Cell Assay); PI3Kα: 12.5 nM (Ki); mTOR: 10.6 nM (Ki)

References

[1] Le PT, et al. Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR. Bioorg Med Chem Lett. 2012 Aug 1;22(15):5098-103. DOI:10.1016/j.bmcl.2012.05.100