Powder: -20°C for 3 years | In solvent: -80°C for 1 year
FM-381 是一种可逆的JAK3共价抑制剂,靶向 Cys909 位点,对 JAK3 的IC50值为127 pM,选择性分别比 JAK1、JAK2 和 TYK2 高 410、2700 和 3600 倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 463 | 现货 | ||
5 mg | ¥ 1,160 | 现货 | ||
10 mg | ¥ 1,660 | 现货 | ||
25 mg | ¥ 3,390 | 现货 | ||
50 mg | ¥ 4,920 | 现货 | ||
100 mg | ¥ 6,880 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,280 | 现货 |
产品描述 | FM381 is a potent covalent reversible inhibitor of JAK3. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively. |
靶点活性 | JAK3:127 pM |
体外活性 | FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909 at the gatekeeper (GK) position +7 in JAK3 exhibited apparent JAK3 IC50 values of 0.127 nM, with 400-, 2700- and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively. FM-381 was found to be inactive in a selectivity panel of frequently hit BRDs (BRD4, BRPF, CECR, FALZ, TAF1, BRD9). FM-381 shows an apparent EC50 of 100 nM in a dose dependent BRET assay and blocks IL2-stimulated (JAK3/JAK1 dependent) STAT5 phosphorylation at 100 nM, but not JAK3 independent IL6-stimulated (JAK1/2/TYK dependent) STAT3 signalling in Human CD4+ T cells up to 1 μM [1]. |
细胞实验 | CD4+ T Cell cytokine stimulation assay is performed. T cells are purified from peripheral blood mononuclear cells from human donors. Equal numbers of cells are incubated for 1 hr with JAK inhibitors (FM381) (0, 10, 50, 100, 300 nM) or DMSO control and stimulated with cytokines for 30 min. The cells are lysed, and the proteins are separated via PAGE and transferred to a polyvinylidene fluoride membrane. The proteins of interest are blotted with specific antibodies and visualized with an infrared imaging system[1]. |
别名 | FM381 |
分子量 | 428.49 |
分子式 | C24H24N6O2 |
CAS No. | 2226521-65-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
DMSO: 12.5 mg/mL (29.17 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3338 mL | 11.6689 mL | 23.3378 mL | 58.3444 mL |
5 mM | 0.4668 mL | 2.3338 mL | 4.6676 mL | 11.6689 mL | |
10 mM | 0.2334 mL | 1.1669 mL | 2.3338 mL | 5.8344 mL | |
20 mM | 0.1167 mL | 0.5834 mL | 1.1669 mL | 2.9172 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。
FM-381 2226521-65-7 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells JAK FM381 inhibit FM 381 Inhibitor Janus kinase inhibitor