Voxtalisib (XL765) 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 (XL765) 抑制 mTORC1 和 mTORC2，IC₅₀s 分别为 160 和 910 nM。

Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC 50 s=39, 113, 9 and 43?nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC 50 =150?nM) and mTOR (IC 50 =157?nM). Voxtalisib (XL765) inhibits mTORC1 and mTORC2 with IC 50 s of 160 and 910 nM, respectively.

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p110γ 9 nM (IC50) p110α 39 nM (IC50

Voxtalisib (XL765) 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 is determined at various concentrations of ATP, revealing Voxtalisib be an ATP-competitive inhibitor with an equilibrium inhibition constant (Ki) value of 13 nM. Voxtalisib 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 (XL765) has relatively weak inhibitory activity toward the class III PI3K vacuolar sorting protein 34 (VPS34; IC50 value of ~9.1 μM). Consistent with its inhibitory activity against purified PI3K proteins, SAR245409 inhibits EGF-i

Oral administration of Voxtalisib (XL765) causes a dose-dependent decrease of phosphorylation of AKT, p70S6K, and S6 in the tumors, reaching a maximum of 84% inhibition of S6 phosphorylation at 30 mg/kg at 4 hours. The dose-response relationships derive from the 4 hours time point predict 50% inhibition of AKT, p70S6K, and S6 phosphorylation to occur at doses of 19 mg/kg (pAKT and pAKT), 51 mg/kg (p-p70S6K), and 18 mg/kg (pS6). Inhibition of AKT, p70S6K, and S6 phosphorylation in MCF7 tumors following a 30 mg/kg dose of Voxtalisib is maximal at 4 hours, reaching 61% to 84%; however, the level of inhibition decreases to 0% to 42% by 24 hours, and minimal or no inhibition is evident by 48 hours. Following a 100 mg/kg dose of Voxtalisib, inhibition is also maximal at 4 hours (52%-75%). has not independently confirmed the a

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[1]. Garcia-Echeverria C, et al. Drug discovery approaches targeting the PI3K/Akt pathway in cancer. Oncogene. 2008 Sep 18;27(41):5511-26.
[2]. Yu P, et al. Characterization of the activity of the PI3K/mTOR inhibitor XL765 (SAR245409) in tumor models with diverse genetic alterations affecting the PI3K pathway. Mol Cancer Ther. 2014 May;13(5):1078-91.

In Vitro: DMSO : 10 mg/mL (37.00 mM; Need ultrasonic)配制储备液