CAS:934493-76-2Voxtalisib

您的位置 : 首页 / PI3K/Akt/mTOR / PI3K / Voxtalisib

Voxtalisib Voxtalisib Cat No. FB01550Cas No. 934493-76-2

Synonyms: XL765;SAR-245409

Voxtalisib is a potent and highly selective inhibitor of class I PI3Ks with IC50 of 39/110/9/43 nM for PI3Kα/β/γ/δ, also inhibits mTOR with IC50 of 160-910 nM.

规格	价格	促销价格	库存

18817579266

立即询价

咨询

18817579266

立即询价

实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.6997 mL
- 18.4987 mL
- 36.9973 mL
- 5 mM
- 0.7399 mL
- 3.6997 mL
- 7.3995 mL
- 10 mM
- 0.3700 mL
- 1.8499 mL
- 3.6997 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号

934493-76-2

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C13H14N6O

运输

蓝冰

分子量

270.29

别名

XL765;SAR-245409

溶解度

DMSO	54.0 mg/mL (199.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

靶点数据

生物活性

靶点 PI3Kβ

IC50:110nM mTOR

IC50:160-910nM PI3Kα

IC50:39nM PI3Kδ

IC50:43nM PI3Kγ

IC50:9nM
描述Activation of the PI3K (phosphoinositide 3-kinase) pathway is a frequent occurrence in human tumors and is thought to promote growth, survival, and resistance to diverse therapies. Voxtalisib (XL765) is a potent and highly selective pan inhibitor of class I PI3Ks (α, β, γ, and δ) with activity against mTOR. In cellular assays, XL765 inhibits the formation of PIP3 in the membrane, and inhibits phosphorylation of AKT, p70S6K, and S6 phosphorylation in multiple tumor cell lines with different genetic alterations affecting the PI3K pathway. XL765 displayed potent inhibitory activity against class I PI3K isoforms p110α, p110β, p110δ, and p120γ, with IC₅₀ values of 39, 110, 43, and 9 nM, respectively, IC₅₀ values of 160 and 910 nM for mTORC1 and mTORC2, respectively. In a vitro study, XL765 inhibits colony growth with an IC₅₀ value of 270 nM in PC-3 cells and 230 nM in MCF7 cells. Oral administration of XL765 (10, 30, 100, or 300 mg/kg) caused a dose-dependent decrease of phosphorylation of AKT, p70S6K, and S6 in the tumors on melanoma xenograft mice, reaching a maximum of 84% inhibition of S6 phosphorylation at 30 mg/kg at 4h.

靶点	Description	IC50
PI3Kβ		IC50:110nM
mTOR		IC50:160-910nM
PI3Kα		IC50:39nM
PI3Kδ		IC50:43nM
PI3Kγ		IC50:9nM