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  • 化合物 JAK3-IN-11|T9811|TargetMol

化合物 JAK3-IN-11|T9811|TargetMol

JAK3-IN-11
10600 25mg 起订
17500 100mg 起订
13800 50mg 起订
上海 更新日期:2025-07-28

TargetMol中国(陶术生物)

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联系人:邵小姐
手机:4008200310 拨打
邮箱:marketing@tsbiochem.com

产品详情:

中文名称:
化合物 JAK3-IN-11
英文名称:
JAK3-IN-11
CAS号:
2412734-00-8
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
产品类别:
抑制剂
货号:
T9811

Product Introduction

Bioactivity

名称JAK3-IN-11
描述JAK3-IN-11 (Compound 12) exhibits potent, noncytotoxic, irreversible, orally active JAK3 inhibitory activity (IC50 = 1.7 nM) with an excellent selectivity profile (>588-fold compared to other JAK isoforms), covalently binds to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T-cell proliferation which is a promising tool for studying autoimmune diseases [1].
体外活性JAK3-IN-11 (Compound 12) (10 μM, 72 h) has no obvious cytotoxicity at a concentration of 10 μM [1]. JAK3-IN-11 (Compound 12) (72 h) shows strong inhibition for T cell proliferation with IC 50 values of 0.83 μM (anti-CD3/CD28 stimulation) and 0.77 μM (IL-2 stimulation) [1]. JAK3-IN-11 (Compound 12) (0-10 μM, 1h) abrogates IL-2 or IL-15-induced phosphorylation of STAT5 in a concentration-dependent manner [1]. JAK3-IN-11 (Compound 12) covalently binds to JAK3 and irreversibly inhibits JAK3 [1]. Cell Proliferation Assay [1] Cell Line: Mouse T cells in complete RPMI1640 medium then exposed to anti-CD3/anti-CD28 or IL-2. Concentration: Incubation Time: 72 h. Result: Displayed strong inhibition for T cell proliferation with an IC 50 values of 0.83 μM (anti-CD3/CD28 stimulation) and 0.77 μM (IL-2 stimulation), showed obvious significant immunosuppressive activity under selective inhibition of JAK3. Western Blot Analysis [1] Cell Line: Purified T cells were pre-activated coated with anti-CD3 and anti-CD28 for 72 h, then cultured with IL-2 (50 U/mL) for 36 h, then, cultured without IL-2 for 36 h Concentration: 0.01, 0.1, 1, 10 μM. Incubation Time: 1 h. Result: Abrogated IL-2 or IL-15-induced phosphorylation of STAT5 in a concentration-dependent manner.
体内活性JAK3-IN-11 (Compound 12) (Oxazolone (OXZ)-induced DTH Balb/c mice; 0-30 mg/kg; PO, prior to and during the challenge phase, 6 days) inhibits oxazolone (OXZ)-induced delayed type hypersensitivity (DTH) responses in a dose-dependent manner [1]. Animal Model: Oxazolone (OXZ)-induced DTH Balb/c mice model [1]. Dosage: 30, 10, and 3 mg/kg. Administration: PO, prior to and during the challenge phase, 6 days. Result: Dose-dependently inhibited oxazolone (OXZ)-induced delayed-type hypersensitivity (DTH) responses. Animal Model: Male ICR mice [1]. Dosage: 30 mg/kg for oral gavage, 10 mg/kg for intravenous administration. Administration: Pharmacokinetic Analysis Result: Preliminary pharmacokinetic data of JAK3-IN-11 (Compound 12) in male ICR Mice [1] Male ICR mice, 30 mg/kg for oral gavage, 10 mg/kg for intravenous administration [1]. Compound 12 iv (10 mg/kg) po (30 mg/kg) AUC(0-t) (mg/L*h) a 1244.41 ± 77.83 889.42 ± 48.32 AUC(0-∞) (mg/L*h) 1274.41 ± 57.18 897.12 ± 56.72 MRT (0-∞) (h) b 0.73 ± 0.08 1.42 ± 0.38 Vz (L/kg) c 8.36 ± 1.83 220.42 ± 24.71 CLz (L/h/kg) d 8.15 ± 1.21 97.14 ± 20.87 t 1/2 (h) e 0.47 ± 0.06 1.52 ± 0.34 C max (mg/L) f 8763.23 ± 324.65 2008.21 ± 189.44 Bioavailability(%) g 23.82% a Area under the concentration time curve. b Mean residence time. c Volume in steady state. d Plasma clearance. e Terminal half-life. f Peak plasma concentrations. g Bioavailability = AUC 0-t (po)/AUC 0-t × 100%.
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
关键字JAK-3-IN-11 | JAK3-IN-11 | JAK3IN11 | JAK3 IN 11
JAK3-IN-11|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (13年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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