PI3Kδ-IN-10

Name: PI3Kδ-IN-10
Brand: TargetMol
SKU: T62013
Price: 255 USD
Availability: InStock
Rating: 4.5 (1 reviews)

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产品编号 T62013Cas号 2409725-49-9

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)。

PI3Kδ-IN-10

还可以

产品编号 T62013Cas号 2409725-49-9

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	库存
25 mg	¥ 10,600	6-8周
50 mg	¥ 13,800	6-8周
100 mg	¥ 17,500	6-8周

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产品介绍

生物活性

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.