ChemicalBook > CAS DataBase List > Pyrido[2,3-d]pyrimidin-7(8H)-one, 2-amino-8-cyclopentyl-4-methyl-6-(1H-pyrazol-4-yl)-

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

Product Name
Pyrido[2,3-d]pyrimidin-7(8H)-one, 2-amino-8-cyclopentyl-4-methyl-6-(1H-pyrazol-4-yl)-
CAS No.
1013098-90-2
Chemical Name
Pyrido[2,3-d]pyrimidin-7(8H)-one, 2-amino-8-cyclopentyl-4-methyl-6-(1H-pyrazol-4-yl)-
Synonyms
PI3KαPI3Kα/mTOR-IN-1;PI3Kα/mTORIN1,PI3Kα/mTOR IN 1,PI-3Kα/mTOR-IN-1;Pyrido[2,3-d]pyrimidin-7(8H)-one, 2-amino-8-cyclopentyl-4-methyl-6-(1H-pyrazol-4-yl)-
CBNumber
CB63339703
Molecular Formula
C16H18N6O
Formula Weight
310.35
MOL File
1013098-90-2.mol
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Pyrido[2,3-d]pyrimidin-7(8H)-one, 2-amino-8-cyclopentyl-4-methyl-6-(1H-pyrazol-4-yl)- Property

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
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Hazard and Precautionary Statements (GHS)

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

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

PI3Kα/mTOR-IN-1 exhibits low HLM ER, but it is highly cleared in rat liver microsome (RLM) with ER of 0.88. PI3Kα/mTOR-IN-1 exhibits moderate clearance, moderate Vdss, T1/2 of 0.9 h, and good oral bioavailability[1].

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

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

Raw materials

Preparation Products

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

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1013098-90-2, Pyrido[2,3-d]pyrimidin-7(8H)-one, 2-amino-8-cyclopentyl-4-methyl-6-(1H-pyrazol-4-yl)-Related Search:


  • Pyrido[2,3-d]pyrimidin-7(8H)-one, 2-amino-8-cyclopentyl-4-methyl-6-(1H-pyrazol-4-yl)-
  • PI3Kα/mTOR-IN-1
  • PI3K&alpha
  • PI3Kα/mTORIN1,PI3Kα/mTOR IN 1,PI-3Kα/mTOR-IN-1
  • 1013098-90-2