Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PI3Kδ-IN-8 is a powerful and specific oral inhibitor of PI3Kδ, exhibiting an IC50 of 3.3 nM. It demonstrates preferential inhibition of PI3Kδ when compared to PI3Kα, PI3Kβ, and PI3Kγ, with IC50 values of 377.2 nM, 241.6 nM, and 17.9 nM, respectively. Furthermore, PI3Kδ-IN-8 possesses notable anti-tumor efficacy.
产品描述 | PI3Kδ-IN-8 is a powerful and specific oral inhibitor of PI3Kδ, exhibiting an IC50 of 3.3 nM. It demonstrates preferential inhibition of PI3Kδ when compared to PI3Kα, PI3Kβ, and PI3Kγ, with IC50 values of 377.2 nM, 241.6 nM, and 17.9 nM, respectively. Furthermore, PI3Kδ-IN-8 possesses notable anti-tumor efficacy. |
靶点活性 | PI3Kγ:17.9 nM (IC50), PI3Kα:377.2 nM (IC50), PI3Kβ:241.6 nM (IC50), PI3Kδ:3.3 nM (IC50) |
体外活性 | PI3Kδ-IN-8 (compound 34) (0.1 nM-10 μM; 96 h) shows excellent potency against representative DLBCL cell lines, of either GCB (SUDHL-6), or ABC subtype (OCI-Ly10 and TMD-8)[1]. PI3Kδ-IN-8 (1 h) inhibits the PI3K-induced AKT phosphorylation in anti-IgM stimulated Raji cells, with an IC 50 of 9.5 nM[1]. Cell Viability Assay[1]Cell Line: SUDHL-6, OCI-Ly10, and TMD-8 cell lines Concentration: 0.1, 1, 10, 100, 1000, 10000 nM Incubation Time: 96 hours Result: Inhibited the viability of SUDHL-6, OCI-Ly10, and TMD-8 cells, with IC 50 s of <0.1 nM, <1 nM, and <0.1 nM, respectively. |
体内活性 | PI3Kδ-IN-8 (1-30 mg/kg; p.o. once daily for 24 d) significantly reduces the tumor volume and tumor weight in a dose-dependent manner in mice[1]. PI3Kδ-IN-8 (1 mg/kg; i.v.) displays a suitable half-life (1 h), C max (2.3 μM) and low clearance (5.6 mL/min/kg) in mice[1]. PI3Kδ-IN-8 (10 mg/kg; p.o.) displays moderate oral bioavailability (39%), C max (7.5 μM), and AUC last (22 μM?h) in mice[1]. Animal Model: Female NOD scid mice were injected OCI-Ly10 cells[1]Dosage: 1, 3, 10, 30 mg/kg Administration: P.o. once daily for 24 days Result: Reduced the tumor volume, with an ED 50 of 6.47 mg/kg. Tumor growth inhibition of 81.95% was seen with a highly significant reduction in both tumor volume and tumor weight. Animal Model: Male BALB/c mice[1]Dosage: 1 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis) Administration: Intravenous administration and oral administration Result: I.v.: t 1/2 =1 h, C max =2.3 μM, CL=5.6 mL/min/kg. P.o.: F=39%, C max =7.5 μM, AUC last =22μM?h. |
别名 | PI3Kδ-IN-8 |
分子量 | 509.521 |
分子式 | C28H21F2N7O |
CAS No. | 2101518-75-4 |
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。
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