中文名稱:PI3Kδ-IN-8 | 英文名稱:PI3Kδ-IN-8 |
CAS:2101518-75-4 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
產(chǎn)品類別: 抑制劑 | |
貨號: T39542 |
名稱 | PI3Kδ-IN-8 |
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. |
體外活性 | 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. |
體內(nèi)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. |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
關(guān)鍵字 | PI3Kdelta-IN-8 | PI3KδIN8 | PI-3Kδ-IN-8 | PI3Kδ IN 8 |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 589.8595萬人民幣 |
員工人數(shù) | 100-500人 | 年營業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 中間體,天然產(chǎn)物,生物化工,化學(xué)試劑,生物技術(shù)服務(wù) | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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