| Identification | Back Directory | [Name]
SAR245409 | [CAS]
934493-76-2 | [Synonyms]
CS-1242
Voxtalisib
XL-765;XL 765
Voxtalisib (XL-765)
Voxtalisib (SAR245409)
SAR245409 (XL765, Voxtalisib)
Voxtalisib (XL765, SAR245409)
Voxtalisib (SAR245409, XL765) Analogue
2-Amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)pyrido[2,3-d]pyrimidin-7(8H)-one
Pyrido[2,3-d]pyrimidin-7(8H)-one, 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-3-yl)- | [Molecular Formula]
C13H14N6O | [MDL Number]
MFCD20276656 | [MOL File]
934493-76-2.mol | [Molecular Weight]
270.29 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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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| Company Name: |
NCE Biomedical Co.,Ltd.
|
| Tel: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0.htm |
| Company Name: |
SPIRO PHARMA
|
| Tel: |
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| Website: |
www.spiropharma.com.cn |
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