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CH5132799

CH5132799 structure

CAS No:
1007207-67-1
Formula:
C15H19N7O3S
Chemical 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]amineCH5132799;5-(7-(Methylsulfonyl)-2-morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-ami
Categories:
Biochemical Engineering > Inhibitors

Description

CH5132799 is a selective class I PI3K inhibitor. CH5132799 inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM.

CH5132799 has been used in trials studying the treatment of Solid Tumors.|PI3K-alpha Inhibitor MEN1611 is an orally bioavailable inhibitor of the class I phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) catalytic subunit alpha (PIK3CA), with potential antineoplastic activity. PI3K alpha inhibitor MEN1611 selectively binds to and inhibits PIK3CA and its mutated forms in the PI3K/Akt (protein kinase B)/mammalian target of rapamycin (mTOR) pathway. This results in both apoptosis and growth inhibition in PIK3CA-expressing tumor cells. By specifically targeting PIK3CA, this agent may be more efficacious and less toxic than pan-PI3K inhibitors. In addition, MEN1611 also targets mutated forms of PI3K gamma (PI3Kg). MEN1611 may stimulate the immune system to restore CD8+ T-cell activation and cytotoxicity. Dysregulation of the PI3K/Akt/mTOR pathway is often found in solid tumors and results in the promotion of tumor cell growth, survival, and resistance to chemo- and radio-therapy. PIK3CA, one of the most frequently mutated oncogenes, encodes the p110-alpha catalytic subunit of the class I PI3K. In most solid tumors, the activation of the PI3K pathway is induced by mutations of PIK3CA.

CH5132799 Basic Attributes

Molecular Weight：

377.42146

Exact Mass：

377.127014

UNII：

JCL936W835

DSSTox ID：

DTXSID40678540

NCI Thesaurus Code：

C158603

Characteristics

PSA：

136

XLogP3：

-0.6

Density：

1.58

Boiling Point：

751.1±70.0 °C(Predicted)

Flash Point：

408.1±35.7 °C

Refractive Index：

1.706

Drug Information

MeSH Entry Terms：

CH 5132799

CH5132799 Use and Manufacturing

To a DMF solution (550 ml) of 4-chloro-7-methanesulfonyl-2-morpholin-4-yl-6, 7-dihydro-5H-pyrrolo[2, 3-d]pyrimidine (57.9 g, 181.6 mmol) prepared according to Example 4, Step A, 2-amino-5-(4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl)pyrimidine (48.2 g, 218.0 mmol), potassium phosphate (42.4 g, 199.8 mmol) and water (30 ml) were added, and degassed under a nitrogen atpmosphere.

Computed Properties

Molecular Weight:377.4
XLogP3:-0.6
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:10
Rotatable Bond Count:3
Exact Mass:377.12700867
Monoisotopic Mass:377.12700867
Topological Polar Surface Area:136
Heavy Atom Count:26
Complexity:587
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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