SAR245409 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

SAR245409 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

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