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Voxtalisib

Chemical Structure : Voxtalisib

CAS No.: 934493-76-2

Voxtalisib (XL765;SAR245409;SAR-245409;XL 765;XL-765)

Catalog No.: PC-44791Not For Human Use, Lab Use Only.

Voxtalisib (XL765, SAR245409) is a potent, highly selective ATP-competitive inhibitor of class I PI3Ks with IC50s of 39/110/43/9 nM for p110α/p110β/p110δ/p120γ.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Voxtalisib (XL765, SAR245409) is a potent, highly selective ATP-competitive inhibitor of class I PI3Ks with IC50s of 39/110/43/9 nM for p110α/p110β/p110δ/p120γ.
Voxtalisib (XL765, SAR245409) also inhibits mTORC1/mTORC2/DNA-PK (IC50=160/910/150 nM) and shows weak inhibitory activity toward VPS34 (IC50=9.1 uM).
Voxtalisib (XL765, SAR245409) inhibits phosphorylation of AKT, p70S6K, and S6 phosphorylation in multiple tumor cell lines.
Voxtalisib (XL765, SAR245409) is orally bioactive in mouse xenograft models.

Physicochemical Properties

M.Wt 270.2899
Formula C13H14N6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 16 mg/mL

Chemical Name/SMILES

Pyrido[2,3-d]pyrimidin-7(8H)-one, 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-3-yl)-

References

1. Yu P, et al. Mol Cancer Ther. 2014 May;13(5):1078-91.

2. Papadopoulos KP, et al. Clin Cancer Res. 2014 May 1;20(9):2445-56.

3. Thijssen R, et al. Leukemia. 2016 Feb;30(2):337-45.

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