Voxtalisib (XL-765) 是一种有效的 PI3K 抑制剂，抑制p110α，p110β，p110γ 和 p110δ，IC50 分别为 39, 113, 9 和 43 nM，也抑制 DNA-PK (IC50=150 nM) 和 mTOR (IC50=157 nM)。Voxtalisib (XL-765) 抑制 mTORC1 和 mTORC2，IC50s 分别为 160 和 910 nM。
CAS：934493-76-2
分子式：C13H14N6O
分子量：270.29
纯度：98%
存储：Store at -20°C

Background:

Voxtalisib (XL-765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC50s=39, 113, 9 and 43 nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC50=150 nM) and mTOR (IC50=157 nM). Voxtalisib (XL-765) inhibits mTORC1 and mTORC2 with IC50s of 160 and 910 nM, respectively. p110γ|9 nM (IC50)|p110α|39 nM (IC50)|p110δ|43 nM (IC50)|p110β|113 nM (IC50)|mTOR|157 nM (IC50)|mTORC1|160 nM (IC50)|mTORC2|910 nM (IC50)|DNA-PK|150 nM (IC50)

Voxtalisib (XL-765) displays potent inhibitory activity against class I PI3K isoforms p110α, p110β, p110δ, and p120γ, with IC50s of 39, 110, 43, and 9 nM, respectively. The IC50 value for inhibition of PI3Kα by Voxtalisib (XL-765) is determined at various concentrations of ATP, revealing Voxtalisib (XL-765) be an ATP-competitive inhibitor with an equilibrium inhibition constant (Ki) value of 13 nM. Voxtalisib (XL-765) also inhibits mTOR (IC50s of 160 and 910 nM for mTORC1 and mTORC2, respectively) in an immune-complex kinase assay and the PI3K-related kinase DNA-PK (IC50 value of 150 nM). In contrast, Voxtalisib (XL-765) has relatively weak inhibitory activity toward the class III PI3K vacuolar sorting protein 34 (VPS34; IC50 value of