| Identification | Back Directory | [Name]
CH5132799 | [CAS]
1007207-67-1 | [Synonyms]
CS-541
100843
CS-1068
CH5132799
CH5132799 (PA-799)
CH5132799 USP/EP/BP
CH5132799;CH 5132799;CH-5132799
5-(7-(Methylsulfonyl)-2-morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-ami
5-(7-methylsulfonyl-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine
5-(7-(Methylsulfonyl)-2-Morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyriMidin-4-yl)pyriMidin-2-aMine
2-Pyrimidinamine, 5-[6,7-dihydro-7-(methylsulfonyl)-2-(4-morpholinyl)-5H-pyrrolo[2,3-d]pyrimidin-4-yl]-
[5-[7-Methylsulfonyl-2-(morpholin-4-yl)-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-yl]amine
CH5132799,5-(7-(Methylsulfonyl)-2-Morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyriMidin-4-yl)pyriMidin-2-aMine
[5-[7-Methylsulfonyl-2-(morpholin-4-yl)-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-yl]amine CH5132799 | [Molecular Formula]
C15H19N7O3S | [MDL Number]
MFCD22419020 | [MOL File]
1007207-67-1.mol | [Molecular Weight]
377.42 |
| Chemical Properties | Back Directory | [Boiling point ]
751.1±70.0 °C(Predicted) | [density ]
1.58 | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Powder | [pka]
3.96±0.20(Predicted) |
| Hazard Information | Back Directory | [Uses]
CH5132799 is a selective class I phosphoinositide 3-kinase (PI3K) inhibitor that targets human cancers harboring oncogenic PIK3CA mutations. CH5132799 also showed potent antiproliferative and antitumor activity. | [Biological Activity]
ch5132799 is an inhibitor of class i phosphatidylinositol 3-kinase (pi3k) with ic50 value of 14nm against pi3kα [1].ch5132799 shows inhibitory effect on class i pi3k with ic50 values of 0.014μm, 0.12μm, 0.5μm and 0.036μm against pi3kα, pi3kβ, pi3kδ and pi3kγ, respectively. pi3kα is especially sensitive to ch5132799. ch5132799 is a selective inhibitor. it shows less effect on class ii pi3ks, class iii pi3k and mtor. for other 26 protein kinases, ch5132799 nearly has no inhibition with ic50 value of > 10μm. ch5132799 is found to have potent antitumor activity. it exerts ic50 values of 0.2μm, 0.032μm, 0.056μm and 0.12μm in hct116, kpl-4, t-47d and sk-ov-3 cell lines, respectively. moreover, ch5132799 is oral available in animal models. treatment of ch5132799 shows strong tumor regression at dose of 12.5 mg/kg in mice bearing human breast cancer xenografts [1]. | [target]
PI3Kα | [storage]
Store at -20°C | [References]
[1] ohwada j, ebiike h, kawada h, et al. discovery and biological activity of a novel class i pi3k inhibitor, ch5132799. bioorganic & medicinal chemistry letters, 2011, 21(6): 1767-1772. |
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