|
| | CH5132799 Basic information |
| Product Name: | CH5132799 | | Synonyms: | CH5132799;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;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;CH5132799;CH 5132799;CH-5132799;5-(7-(Methylsulfonyl)-2-morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-ami;CS-541 | | CAS: | 1007207-67-1 | | MF: | C15H19N7O3S | | MW: | 377.42 | | EINECS: | | | Product Categories: | Inhibitors;PI3K/Akt/mTOR;JAK;STAT;Akt;mTOR;PI3K | | Mol File: | 1007207-67-1.mol |  |
| | CH5132799 Chemical Properties |
| 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) |
| | CH5132799 Usage And Synthesis |
| 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 | | 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. |
| | CH5132799 Preparation Products And Raw materials |
|
