| Identification | Back Directory | [Name]
Pyrido[2,3-d]pyrimidin-7(8H)-one, 2-amino-8-cyclopentyl-4-methyl-6-(1H-pyrazol-4-yl)- | [CAS]
1013098-90-2 | [Synonyms]
PI3K&alpha
PI3Kα/mTOR-IN-1
PI3Kα/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)- | [Molecular Formula]
C16H18N6O | [MDL Number]
MFCD31544429 | [MOL File]
1013098-90-2.mol | [Molecular Weight]
310.35 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
|