CH5132799 ( CH5132799; CH-5132799; PA799; PA-799. )

Catalog No. M17113 CAS No. 1007207-67-1

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Product Name

CH5132799
Note

Research use only, not for human use.
Brief Description

CH5132799 has been used in trials studying the treatment of Solid Tumors.
Description

CH5132799, also known as PA-799, is a novel class I PI3K inhibitor, which exhibited a strong inhibitory activity especially against PI3Kα (IC(50)=0.014 μM). In human tumor cell lines with PI3K pathway activation, CH5132799 showed potent antiproliferative activity. CH5132799 is orally available and showed significant antitumor activity in PI3K pathway-activated human cancer xenograft models in mice. CH5132799 selectively inhibited class I PI3Ks and PI3Kα mutants in in vitro kinase assays. Tumors harboring PIK3CA mutations were significantly sensitive to CH5132799 in vitro and were remarkably regressed by CH5132799 in in vivo mouse xenograft models.
Synonyms

CH5132799; CH-5132799; PA799; PA-799.
Pathway

Others
Target

Other Targets
Recptor

mTOR; PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ
Research Area

Cancer
Indication

——

CAS Number

1007207-67-1
Formula Weight

377.42
Molecular Formula

C15H19N7O3S
Purity

98%
Solubility

DMSO : 4.55 mg/mL 12.06 mM;H2O : < 0.1 mg/mL
SMILES

CS(=O)(=O)N1CCc2c(nc(nc12)N1CCOCC1)c1cnc(N)nc1
Chemical Name

5-(7-(methylsulfonyl)-2-morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine

1. Tanaka H, et al, Clin Y Res, 2011, 17(10), 3272-3281.

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