SAR245409

Product NameSAR245409
CAS934493-76-2
MFC13H14N6O
MW270.29
EINECS
MOL File934493-76-2.mol

Chemical Properties

Boiling point	605.0±65.0 °C(Predicted)
Density	1.397±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO : 10 mg/mL (37.00 mM; Need ultrasonic)
form	Powder
pka	12.54±0.10(Predicted)
color	Off-white to brown

Safety Information

HS Code

29337900

Usage And Synthesis

Definition

ChEBI: 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinone is a pyrazolopyridine.

Biological Activity

Voxtalisib (SAR245409, XL765) is a dual mTOR/PI3K inhibitor with the strongest effect on p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.

in vitro

Voxtalisib (XL765) is the first oral dual inhibitor of PI3K and mTOR with IC50 of 39, 113, 9, 43, and ~150 nM for p110α, β, γ, δ, and mTOR, respectively. In vitro, XL765 decreased cell viability in a concentration-dependent manner.

in vivo

Oral feeding of XL765 resulted in a 12-fold increase in the number of mid-stage tumor declines compared to the control group. XL765 showed activity either alone or in combination with other drugs in various GBM xenografts. XL765 induces downregulation of PI3K downstream phosphorylated proteins: pAkt and pPRAS40, and mTOR downstream phosphorylated proteins: pS6 and p4EBP1 in cultured human xenograft tumors in vitro.

target

PI3Kγ

Preparation Products And Raw materials

Raw materials

6-bromo-8-ethyl-4-methyl-2-methylsulfanylpyrido[2,3-d]pyrimidin-7-one 5-Pyrimidinecarboxylic acid, 4-(ethylamino)-6-methyl-2-(methylthio)-, ethyl ester Pyrido[2,3-d]pyrimidin-7(8H)-one, 2-amino-6-bromo-8-ethyl-4-methyl-5-Pyrimidinecarboxaldehyde, 4-(ethylamino)-6-methyl-2-(methylthio)-5-Pyrimidinemethanol, 4-(ethylamino)-6-methyl-2-(methylthio)-2-amino-8-ethyl-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one 8-ethyl-4-methyl-2-methylsulfanyl-6-(1H-pyrazol-5-yl)pyrido[2,3-d]pyrimidin-7-one 8-Ethyl-4-methyl-2-(methylthio)pyrido[2,3-d]pyrimidin-7(8H)-one N-ethyl-5-iodo-6-methyl-2-(methylthio)pyrimidin-4-amine 2-amino-4-methyl-6-ethylaminopyrimidine Ethyl 4-Chloro-6-methyl-2-(methylthio)pyrimidine-5-carboxylate 6-Methyl-2-(methylthio)pyrimidin-4-ol 4-Chloro-6-methyl-2-(methylthio)pyrimidine