Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Sonidegib (Erismodegib) 是一种Smo 的选择性拮抗剂,能够抑制鼠 Smo (IC50:1.3 nM)和人 Smo (IC50:2.5 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 538 | 现货 | ||
10 mg | ¥ 832 | 现货 | ||
25 mg | ¥ 1,557 | 现货 | ||
50 mg | ¥ 2,480 | 现货 | ||
100 mg | ¥ 3,730 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 593 | 现货 |
产品描述 | Sonidegib (Erismodegib), a Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively. |
靶点活性 | Smo (mouse):1.3 nM, Smo (human):2.5 nM |
体外活性 | PAMPA实验显示,LDE225的渗透性可达90.8%.在临床物种的梯度稀释试验中,LDE225表现出良好的口服药效率,生物药效率为69%-102%.LDE225呈弱碱性(pKa:4.20),且其水溶性也相对较差.LDE225有剂量依赖性的抗肿瘤活性.LDE225与大鼠,小鼠以及人源的血浆蛋白的结合能力很强(>99%),且可与狗和猴子的血浆蛋白结合,结合能力分别是77%和 85%.在Rip1-Tag2小鼠体内,LDE225可显著减少95.7%的肿瘤体积.LDE225(5 mg/kg/天)显著抑制肿瘤生长,与33%的T/C值相同.LDE225(10或20 mg/kg/天)促使肿瘤退化的效果分别达到51%和83%.Gli1 mRNA抑制性与LDE225介导的肿瘤与血浆接触有关.在肿瘤移植的动物模型中,经过四天的给药处理,LDE225可成功透过血脑屏障抑制肿瘤生长. |
体内活性 | LDE 225(0.6-0.8 μM)可抑制TM3荧光报告细胞系(经1 nM-25 nM Hh激动剂Ag1.5 处理)。 |
细胞实验 | LDE225 is prepared for assay by serial dilution in DMSO and then added to empty assay plates. TM3Hh12 cells (TM3 cells containing Hh-responsive reporter gene construct pTA-8xGli-Luc) are cultured in F12 Ham's/DMEM (1:1) containing 5% horse serum, 2.5% fetal bovine serum (FBS), and 15 mM HEPES, pH 7.3. Cells are harvested by trypsin treatment, resuspended in F12 Ham's/DMEM (1:1) containing 5% horse serum and 15 mM HEPES, pH 7.3, added to assay plates, and incubated with LDE225 for approximately 30 min at 37 °C in 5% CO2. Then 1 nM or 25 nM Ag1.5 is added to assay plates and incubated at 37 °C in the presence of 5% CO2. After 48 hours, either Bright-Glo or MTS reagent is added to the assay plates and luminescence or absorbance at 492 nm is determined. IC50 values, defined as the inflection point of the logistic curve, are determined by nonlinear regression of the Gli-driven luciferase luminescence or absorbance signal from MTS assay vs log10 (concentration) of LDE225 using the R statistical software pack (Only for Reference) |
别名 | Erismodegib, NVP-LDE225, LDE225 |
分子量 | 485.5 |
分子式 | C26H26F3N3O3 |
CAS No. | 956697-53-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90 mg/mL (185.4 mM)
Ethanol: 90 mg/mL (185.4 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 / Ethanol | 1 mM | 2.0597 mL | 10.2987 mL | 20.5973 mL | 51.4933 mL |
5 mM | 0.4119 mL | 2.0597 mL | 4.1195 mL | 10.2987 mL | |
10 mM | 0.206 mL | 1.0299 mL | 2.0597 mL | 5.1493 mL | |
20 mM | 0.103 mL | 0.5149 mL | 1.0299 mL | 2.5747 mL | |
50 mM | 0.0412 mL | 0.206 mL | 0.4119 mL | 1.0299 mL | |
100 mM | 0.0206 mL | 0.103 mL | 0.206 mL | 0.5149 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。
Sonidegib 956697-53-3 GPCR/G Protein Stem Cells Hedgehog/Smoothened Smo NVP-LDE-225 LDE-225 Erismodegib Inhibitor inhibit Smoothened LDE 225 NVP-LDE225 NVP-LDE 225 LDE225 inhibitor