Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PI3Kδ-IN-10 是高效的、具有口服活性的PI3Kδ抑制剂(IC50= 2 nM)。在肝细胞癌模型中,PI3Kδ-IN-10 强烈抑制下游AKT 通路,并诱导细胞凋亡(apoptosis)。
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 | PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor (IC50= 2 nM). In hepatocellular carcinoma models, PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis. |
体外活性 | PI3Kδ-IN-10 (compound 9x) (0-10 μM; 72 hours) has cell proliferation inhibitory effects in HCC cell lines with IC 50 of 0.53 - 1.36 μM [1]. PI3Kδ-IN-10 (0-50 μM; 24 hours) markedly enhances expression level of cleaved PARP and cleaved caspase-3, also reduces the level of Akt phosphorylation at Ser473 and Thr308 in a dose-dependent manner [1]. Cell Proliferation Assay Cell Line: Bel-7402, HepG2, Hep3B [1] Concentration: 0-10 μM Incubation Time: 72 hours Result: Showed cell proliferation inhibitory effects in HCC cell lines with IC 50 of 0.53 - 1.36 μM. Western Blot Analysis Cell Line: Bel-7402, HepG2 [1] Concentration: 0 μM, 1.56 μM, 3.12 μM, 6.25 μM, 12.5 μM, 50 μM Incubation Time: 24 hours Result: Markedly enhanced expression level of cleaved PARP and cleaved caspase-3, also reduced the level of Akt phosphorylation at Ser473 and Thr308 in a dose-dependent manner. |
体内活性 | PI3Kδ-IN-10 (5 mg/kg for PO, 1 mg/kg for IV, single) exhibits an acceptable half-life (T 1/2 ), a moderate distribution volume, and acceptable oral bioavailability [1]. PI3Kδ-IN-10 (40 and 20 mg/kg; IV, for 12 days) effectively suppress the growth of live cancer xenografts with inhibition ratios of 76.02% and 59.15% at 40 mg/kg and 20 mg/kg [1]. Pharmacokinetic Parameters of PI3Kδ-IN-10 in female Balb/c (nu/nu) mice [1]. PO (5 mg/kg) IV (1 mg/kg) T 1/2 (h) 2.502 1.131 AUC (h·μg/L) 3067.94 2791.37 Vz/F (L/kg) 6.15 0.587 T max (h) 3 0.083 F (%) 22.0 Animal Model: Female Balb/c (nu/nu) mice [1] Dosage: 5 mg/kg or 1 mg/kg Administration: PO and IV, single (Pharmacokinetic Analysis) Result: Exhibited an acceptable half-life (T 1/2 ), a moderate distribution volume, and acceptable oral bioavailability. Animal Model: Female Balb/c (nu/nu) mice (6 weeks) [1] Dosage: 40 and 20 mg/kg Administration: IV, for 12 days Result: Effectively suppressed the growth of live cancer xenografts with inhibition ratios of 76.02% and 59.15% at 40 mg/kg and 20 mg/kg. |
分子量 | 405.84 |
分子式 | C19H16ClN9 |
CAS No. | 2409725-49-9 |
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。
PI3Kδ-IN-10 2409725-49-9 Inhibitor inhibitor inhibit