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Voxtalisib

Voxtalisib

产品编号 T7014   CAS 934493-76-2
别名: XL765, SAR245409

Voxtalisib (XL765) 是一种PI3K 抑制剂,抑制p110α,p110β,p110γ和p110δ。它抑制mTORC1和mTORC2,IC50s 分别为 160 和 910 nM。它也抑制 DNA-PK (其 IC50=150 nM) 和 mTOR (其 IC50=157 nM)。

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Voxtalisib Chemical Structure
Voxtalisib, CAS 934493-76-2
规格 价格/CNY 货期 数量
1 mg ¥ 438 现货
2 mg ¥ 639 现货
5 mg ¥ 987 现货
10 mg ¥ 1,620 现货
25 mg ¥ 3,280 现货
50 mg ¥ 4,820 现货
100 mg ¥ 6,690 现货
1 mL * 10 mM (in DMSO) ¥ 983 现货
其他形式的 Voxtalisib:
产品目录号及名称: Voxtalisib (T7014)
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纯度: 99.36%
纯度: 99.24%
纯度: 98.01%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Voxtalisib (XL765) (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
靶点活性 p110γ:9 nM
体外活性 XL765 is active against class I PI3K (IC50 = 39, 113, 9 and 43 nM for p110α, β, γ and δ, respectively). XL765 also inhibits DNA-PK (IC50 = 150 nM) and mTOR (IC50 = 157 nM) but not XL-147 which shows IC50 values of > 15 μM. [1] XL765 treatment results in decreased cell viability in 13 PDA cell lines in a dose-dependent manner. XL765, a dual-target PI3K/mTOR inhibitor, inhibits cell growth and apoptosis in many more cell lines and at lower concentrations as compared to the PI3K-selective inhibitors XL147 and PIK90. The effect can be recapitulated by using combinations of single-targeted compounds. XL765 significantly reduces phosphorylation of the mTOR targets S6, S6K, and 4EBP1, which is associated with greater apoptosis induction rather than to PI3K inhibition alone. XL765 treatment causes accumulation of autophagosomes in MIAPaCa-2 cells, and results in significant dose-dependent AVO induction and LC3-II stimulation in MIAPaCa-2 cells stably expressing a LC3-GFP construct. [2]
体内活性 The combination of XL765 (30 mg/kg) with chloroquine (50 mg/kg) results in significant inhibition of BxPC-3 xenograft growth in mice models, while XL765 alone at the same dose has no inhibitory effect. [2] Oral administration of XL765 results in greater than 12-fold reduction in median tumor bioluminescence compared to control and improvement in median survival in nude mice implanted intracranially with GBM 39-luc cells. XL765 in combination with temozolomide (TMZ) yields a 140-fold reduction in median bioluminescence with a trend toward improvement in median survival compared with TMZ alone. [3]
细胞实验 Cells are treated with XL765 24 hours after plating and harvested for apoptosis or autophagy assays at 24, 48, or 72 hours after XL765 treatment. Apoptosis is determined by total percentage of annexin V-positive cells by fluorescence-activated cell sorting (FACS). Acidic vesicular organelles (AVOs) are detected in XL765-treated cells by vital staining with acridine orange. The degree of AVO formation is expressed as fold increase of acridine orange fluorescence intensity (FL3) in XL765-treated cells versus control cells. (Only for Reference)
别名 XL765, SAR245409
分子量 270.29
分子式 C13H14N6O
CAS No. 934493-76-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 50 mg/mL (185 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6997 mL 18.4986 mL 36.9973 mL 92.4932 mL
5 mM 0.7399 mL 3.6997 mL 7.3995 mL 18.4986 mL
10 mM 0.37 mL 1.8499 mL 3.6997 mL 9.2493 mL
20 mM 0.185 mL 0.9249 mL 1.8499 mL 4.6247 mL
50 mM 0.074 mL 0.37 mL 0.7399 mL 1.8499 mL
100 mM 0.037 mL 0.185 mL 0.37 mL 0.9249 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Garcia-Echeverria C, et al. Oncogene, 2008, 27(41), 5511-5526. 2. Mirzoeva OK, et al. J Mol Med, 2011, 89(9), 877-889. 3. Prasad G, et al. Neuro Oncol, 2011, 13(4), 384-392.
IC 86621 (R)-(-)-Rolipram DNA-PK-IN-10 STL127705 Pictilisib dimethanesulfonate Samotolisib PIK-75 hydrochloride PI-103

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌药物库 抗癌临床化合物库 PI3K/Akt/mTOR 化合物库 抗抑郁症化合物库 抗衰老化合物库 激酶抑制剂库 肿瘤免疫治疗小分子化合物库 药物功能重定位化合物库 干细胞分化化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Voxtalisib 934493-76-2 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling mTOR PI3K DNA-PK SAR-245409 inhibit Phosphoinositide 3-kinase Mammalian target of Rapamycin XL-765 XL765 SAR245409 Inhibitor SAR 245409 XL 765 inhibitor

 

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