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SAR245409

CAS No.
934493-76-2
Chemical Name:
SAR245409
Synonyms
CS-1242;Voxtalisib;XL-765;XL 765;Voxtalisib (XL-765);Voxtalisib (SAR245409);Voxtalisib (XL765, SAR245409);SAR245409 (XL765, Voxtalisib);Voxtalisib (SAR245409, XL765) Analogue;2-Amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)pyrido[2,3-d]pyrimidin-7(8H)-one;2-Amino-8-ethyl-4-methyl-6-(1H-pyrazol-3-yl)pyrido[2,3-d]pyrimidin-7(8H)-one
CBNumber:
CB62715669
Molecular Formula:
C13H14N6O
Molecular Weight:
270.29
MDL Number:
MFCD20276656
MOL File:
934493-76-2.mol
MSDS File:
SDS
Last updated:2023-06-08 09:03:02

SAR245409 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)
FDA UNII CVL1685GPH

SAFETY

Risk and Safety Statements

SAR245409 price More Price(18)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 30323 Voxtalisib 934493-76-2 5mg $117 2024-03-01 Buy
Cayman Chemical 30323 Voxtalisib 934493-76-2 50mg $578 2024-03-01 Buy
Cayman Chemical 30323 Voxtalisib 934493-76-2 10mg $176 2024-03-01 Buy
Cayman Chemical 30323 Voxtalisib 934493-76-2 25mg $347 2024-03-01 Buy
ChemScene CS-3163 Voxtalisib 99.46% 934493-76-2 5mg $84 2021-12-16 Buy
Product number Packaging Price Buy
30323 5mg $117 Buy
30323 50mg $578 Buy
30323 10mg $176 Buy
30323 25mg $347 Buy
CS-3163 5mg $84 Buy

SAR245409 Chemical Properties,Uses,Production

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

17119-73-2
934493-76-2
Synthesis of SAR245409 from 4-Chloro-6-methyl-2-(methylthio)pyrimidine
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934493-76-2(SAR245409)Related Search:

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