Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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)。
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 50 mg/mL (185 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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