Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LSD1-IN-14, a powerful and specific inhibitor of LSD1 (with an IC50 value of 0.89 μM), effectively suppresses the growth of A549 and THP-1 cells and promotes the apoptosis of tumor cells [1].
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | LSD1-IN-14, a powerful and specific inhibitor of LSD1 (with an IC50 value of 0.89 μM), effectively suppresses the growth of A549 and THP-1 cells and promotes the apoptosis of tumor cells [1]. |
体外活性 | LSD1-IN-14 (compound x43) (0-20 μM; 72 hours) has a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC 50 values of 1.62 μM and 1.21 μM, respectively [1]. LSD1-IN-14 (0-3 μM;72 hours) significantly upregulates the expression of substrate H3K4me2 and H3K9me2 in a dose-dependent manner [1]. LSD1-IN-14 (0-3 μM;72 hours) induces the apoptosis of 53.6% of A549 cells in a dose-dependent manner [1]. LSD1-IN-14 (1 mM; 60 minutes) has excellent stability in human liver microsomes and weak CYP inhibition, with T 1/2 of 103.3 min and Cl int(mic) of 13.4 μL/min/mg [1]. Cell Proliferation Assay Cell Line: A549 and THP-1 [1] Concentration: 0-20 μM Incubation Time: 72 hours Result: Showed a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, respectively. Western Blot Analysis Cell Line: A549 cells [1] Concentration: 0, 0.3, 1 and 3 μM Incubation Time: 72 hours Result: Significantly upregulated the expression of substrate H3K4me2 and H3K9me2 in a dose-dependent manner. Apoptosis Analysis Cell Line: A549 cells [1] Concentration: 0, 0.3, 1 and 3 μM Incubation Time: 72 hours Result: Induced the apoptosis of 53.6% of cells in a dose-dependent manner. |
体内活性 | LSD1-IN-14 (2 mg/kg for i.v., 10 mg/kg for i.g, single) has an acceptable half-life and oral bioavailability [1]. Pharmacokinetic Parameters of LSD1-IN-14 in male Sprague-Dawley rats [1]. IV (2 mg/kg) IG (10 mg/kg) C 0 (ng/mL) 575 C max (ng/mL) 41.1 T 1/2 (h) 1.0 T 1/2 (h) 2.8 Vd ss (L/kg) 6.6 T max (h) 0.8 Cl (mL/min/kg) 156 AUC 0-t (ng.h/mL) 126 AUC 0-t (ng.h/mL) 211 AUC 0-∞ (ng.h/mL) 152 AUC 0-∞ (ng.h/mL) 214 Bioacailability (%) 11.9 Animal Model: Male Sprague-Dawley rats [1] Dosage: 2 mg/kg for i.v., 10 mg/kg for i.g. Administration: i.v. and i.g, single Result: Showed an acceptable half-life and oral bioavailability. |
分子量 | 365.45 |
分子式 | C21H24FN5 |
CAS No. | 2698340-11-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
LSD1-IN-14 2698340-11-1 Inhibitor inhibitor inhibit