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Akt &GSK-3

CH5132799 (1007207-67-1)

CH5132799 inhibits class I PI3Ks, particularly PI3Kα with IC50 of 14 nM; less potent to PI3Kβδγ, while sensitive in PIK3CA mutations cell lines.

Not Intended for Therapeutic Use. For research use only.

CAS: 1007207-67-1 Category

CH5132799 (1007207-67-1) 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.

CH5132799 (1007207-67-1) Specifications:

Product Name CH5132799
Synonym CH5132799; CH-5132799; CH 5132799; PA-799; PA799; PA-799.
Chemical Name 5-(7-(methylsulfonyl)-2-morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine
Drug Class Antineoplastics
Purity ≥98% (HPLC)
CAS Number 1007207-67-1
Molecular Formula C15H19N7O3S
Molecular Weight 377.42146
Monoisotopic Mass 377.12701 g/mol
MDL number MFCD22419020
InChIKey JEGHXKRHKHPBJD-UHFFFAOYSA-N
InChi Code InChI=1S/C15H19N7O3S/c1-26(23,24)22-3-2-11-12(10-8-17-14(16)18-9-10)19-15(20-13(11)22)21-4-6-25-7-5-21/h8-9H,2-7H2,1H3,(H2,16,17,18)
SMILES NC1=NC=C(C2=C3C(N(S(=O)(C)=O)CC3)=NC(N4CCOCC4)=N2)C=N1
Form Powder
Color White
Solubility  Soluble in DMSO, not soluble in water
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months)
Shelf life >5 years if stored properly
Handling Protect from air and moisture
Application CH5132799 is a novel class I PI3K inhibitor

 


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