Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JANEX-1 (Jak3 inhibitor I) 是一种特异性JAK3抑制剂,Ki 和IC50分别为 2.3 和 78 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 315 | 现货 | ||
2 mg | ¥ 448 | 现货 | ||
5 mg | ¥ 786 | 现货 | ||
10 mg | ¥ 1,380 | 现货 | ||
25 mg | ¥ 2,150 | 现货 | ||
50 mg | ¥ 2,980 | 现货 | ||
100 mg | ¥ 4,290 | 现货 | ||
500 mg | ¥ 8,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 798 | 现货 |
产品描述 | JANEX-1 (Jak3 inhibitor I) is a cell-permeable, reversible, effective, ATP-competitive, and selective inhibitor of JAK3 (IC50: 78 μM); little inhibitory against JAK1/2, or Zap/Syk or SRC tyrosine kinases. |
靶点活性 | JAK3:78 μM |
体外活性 | JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC50 of 78 μM), does not inhibit JAK1 and JAK2, the ZAP/SYK family tyrosine kinase SYK, the TEC family tyrosine kinase BTK, the SRC family tyrosine kinase LYN, or the receptor family tyrosine kinase insulin receptor kinase, even at concentrations as high as 350 μM. JANEX-1 induces apoptosis in JAK3-expressing human leukemia cell lines NALM-6 and LC1;19 but not in melanoma (M24-MET) or squamous carcinoma (SQ20B) cells. WHI-P131 inhibits the clonogenic growth of JAK3-positive leukemia cell lines DAUDI, RAMOS, LC1;19, NALM-6, MOLT-3, and HL-60 (but not JAK3-negative BT-20 breast cancer, M24-MET melanoma, or SQ20B squamous carcinoma cell lines) in a concentration-dependent fashion. WHI-P131 inhibits clonogenic growth in a concentration-dependent fashion with EC50s of 24.4 μM for NALM-6 cells and 18.8 μM for DAUDI cells. At 100 μM, WHI-P131 inhibits the in vitro colony formation by these leukemia cell lines by >99%. In contrast, JANEX-1 does not inhibit the clonogenic growth of JAK3-negative M24-MET melanoma or SQ20B squamous carcinoma cell lines[1]. |
体内活性 | JANEX-1 is administered at doses ranging from 5 to 100?mg/kg. Evaluation of CPK activity revealed a dose-response curve with an effective dose 50 (ED50) value of 7.44?mg/kg. Mice receiving JANEX-1 displayed significantly reduced CPK and LDH levels. In addition, the infarct size of JANEX-1-treated mice (30.16±2.79%) is significantly decreased when compared with I/R-operated mice (65.64±3.76%)[2]. JANEX-1 (WHI-P131) is absorbed rapidly, and the time to reach the maximum plasma JANEX-1 concentration (tmax) is 24.7±1.7 min. JANEX-1 is rapidly eliminated with an elimination half-life of 45.6±5.5 min. Although the predicted maximum plasma JANEX-1 concentration is 10.5 ± 0.8 μM, which is only half of the Cmax following i.v. administration of the same bolus dose, the i.p. bioavailability is 94.6% and the systemic exposure levels (i.e., AUC) are very similar to those observed after i.v. injection (17.1±2.2 μM?h versus 18.1±1.2 μM?h)[3]. |
细胞实验 | JANEX-1 (WHI-P131) is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO 0.1%) before use[1]. The following cell lines are used in various biological assays: NALM-6 (pre-B-ALL), LC1;19 (pre-B-ALL), DAUDI (B-ALL), RAMOS (B-ALL), MOLT-3 (T-cell ALL), HL60 (acute myelogenous leukemia), BT-20 (breast cancer), M24-MET (melanoma), SQ20B (squamous cell carcinoma), and PC3 (prostate cancer). These cell lines are maintained in culture. Cells are seeded in six-well tissue culture plates at a density of 50×104 cells/well in a treatment medium containing various concentrations of JANEX-1 (0.1, 0.2, 0.3, 0.4 and 0.5 nM) and incubated for 24-48 h at 37°C in a humidified 5% CO2 atmosphere. Cells are examined for apoptotic changes after treatment with JANEX-1 by the in situ TdT-mediated dUTP end-labeling assay using the ApopTag apoptosis detection kit[1]. |
别名 | Jak3 inhibitor I, WHI-P131 |
分子量 | 297.31 |
分子式 | C16H15N3O3 |
CAS No. | 202475-60-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (184.99 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.3635 mL | 16.8175 mL | 33.6349 mL | 84.0873 mL |
5 mM | 0.6727 mL | 3.3635 mL | 6.727 mL | 16.8175 mL | |
10 mM | 0.3363 mL | 1.6817 mL | 3.3635 mL | 8.4087 mL | |
20 mM | 0.1682 mL | 0.8409 mL | 1.6817 mL | 4.2044 mL | |
50 mM | 0.0673 mL | 0.3363 mL | 0.6727 mL | 1.6817 mL | |
100 mM | 0.0336 mL | 0.1682 mL | 0.3363 mL | 0.8409 mL |
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。
JANEX-1 202475-60-3 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells JAK inhibit WHI-P 131 Janus kinase JANEX1 JANEX 1 Inhibitor Jak3 inhibitor I WHI-P131 WHI-P-131 inhibitor