keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LCL161 是一种 SMAC 模拟物,可有效结合并抑制多种 IAP。它抑制 HEK293 细胞中 XIAP 和 MDA-MB-231细胞中 cIAP1的 IC50分别为 35 和 0.4 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 418 | 现货 | ||
5 mg | ¥ 645 | 现货 | ||
10 mg | ¥ 997 | 现货 | ||
25 mg | ¥ 1,997 | 现货 | ||
50 mg | ¥ 3,437 | 现货 | ||
100 mg | ¥ 3,990 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 711 | 现货 |
产品描述 | LCL161, a SMAC mimetic, effectivity binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP). |
靶点活性 | XIAP (HEK293 cells):35 nM, CIAP1 (MDA-MB-231 cells):0.4 nM |
体外活性 | 尼罗替尼与LCL161联用对白血病生长的抑制具有累加作用.LCL161(100 mg/kg)增强尼罗替尼(100 mg/kg)对患有白血病小鼠的体内作用.LCL161使PKC412对Ba/F3-FLT3-ITD-luc+细胞体内生长的抑制作用显著增强.LCL161能够与阿霉素和阿糖胞苷(标准化疗剂)阳性结合,抗FLT3-ITD和D835Y表达细胞. |
体内活性 | LCL161可适度抑制表达FLT3-ITD的细胞生长,IC50的范围为0.5 μM (Ba/F3-FLT3-ITD 细胞)到4 μM (MOLM13-luc+ 细胞)。LCL161对D835Y突变体的抑制能力相当高,测试抗Ba/F3-D835Y细胞时,IC50为50 nM。LCL161与凋亡抑制蛋白因子的结合亲和力高,且可启动对cIAP1/2的破坏,其激活胱天蛋白酶后进而诱导细胞凋亡。LCL161 与PKC412联用对MOLM13-luc+细胞的细胞杀伤力要强于其任何一个单独使用的药剂,Calcusyn复合指数表明其具有协同作用。 |
激酶实验 | CYP3A activity is assessed using the probe reactions, midazolam-1′-hydroxylation and testosterone 6β-hydroxylation. For reversible inhibition, incubations (37°C, 10 min) are composed of (final concentrations): potassium phosphate buffer (100 mM, pH 7.4), β-NADPH (1 mM), magnesium chloride (5 mM), microsomal protein (0.025 mg/mL), probe substrate (1 μM midazolam or 25 μM testosterone), LCL161 (0, 0.5, 1, 5, 10, 25, 50, or 100 μM) and organic solvent (0.2% acetonitrile for midazolam, 0.2% methanol for testosterone). After a 3-minute preincubation, the reactions are initiated by addition of β-NADPH and terminated by addition of acetonitrile (two volumes). Reactions are previously shown to be linear with respect to time and protein concentration (results not shown) with midazolam and testosterone turnover of 8.7±1.3% (n=3) and 2.6±0.20%, respectively. Formation of 1′-hydroxymidazolam and 6β-hydroxytestosterone is determined by LC-MS/MS as described below[3]. |
细胞实验 | In vitro testing is performed using DIMSCAN (Only for Reference) |
分子量 | 500.63 |
分子式 | C26H33FN4O3S |
CAS No. | 1005342-46-0 |
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (185.8 mM)
Ethanol: 16 mg/mL (32 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 | 1.9975 mL | 9.9874 mL | 19.9748 mL | 49.9371 mL |
5 mM | 0.3995 mL | 1.9975 mL | 3.995 mL | 9.9874 mL | |
10 mM | 0.1997 mL | 0.9987 mL | 1.9975 mL | 4.9937 mL | |
20 mM | 0.0999 mL | 0.4994 mL | 0.9987 mL | 2.4969 mL | |
DMSO | 50 mM | 0.0399 mL | 0.1997 mL | 0.3995 mL | 0.9987 mL |
100 mM | 0.02 mL | 0.0999 mL | 0.1997 mL | 0.4994 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。
LCL161 1005342-46-0 Apoptosis IAP inhibit Inhibitor LCL-161 LCL 161 inhibitor