化合物 PI3Kδ-IN-10 T62013

Product Introduction
Bioactivity


英文名: PI3Kδ-IN-10

描述: 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)。

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途