Powder: -20°C for 3 years | In solvent: -80°C for 1 year
XL019 是一种具有口服活性的选择性JAK2抑制剂。它对JAK2的选择性是 100 多种丝氨酸/苏氨酸和酪氨酸激酶的 50 倍以上。它对 JAK2 V617F 和野生型 JAK2 细胞中 STAT3 和 STAT5 磷酸化有抑制作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 245 | 现货 | ||
5 mg | ¥ 622 | 现货 | ||
10 mg | ¥ 980 | 现货 | ||
25 mg | ¥ 1,930 | 现货 | ||
50 mg | ¥ 3,490 | 现货 | ||
100 mg | ¥ 5,120 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 683 | 现货 |
产品描述 | XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1. |
靶点活性 | JAK2:2.2 nM |
体外活性 | XL019具有优越的药效学特性,并且表现出良好的口服吸收性,在不同物种中表现适中的清除率和半衰期.在给药30,100和300 mg/kg XL019后,明显抑制下游标记pSTAT1和pSTAT3,导致pSTAT1的ED 50为42 mg/kg和pSTAT3的ED 50为210 mg/kg.XL019抑制小鼠HEL.92.1.7异种移植肿瘤生长,200 mg/kg和300 mg/kg XL019分别每天给药两次持续14天,表现60%和70%的抑制作用. |
体内活性 | L019抑制JAK2以及突变形式JAK2V617F的激活,其可导致JAK-STAT信号传导途径的抑制并可诱导凋亡。与其他细胞系统相比,在EPO刺激红细胞系后,XL019显示出10倍以上的STAT5磷酸化选择性抑制(IC50 = 64 nM)。 |
激酶实验 | FRET-Based Z′-Lyte Assay Detecting Peptide Substrate Phosphorylation: The kinases ABL1, ABL1(E255K), ABL1 (G250E), ABL1(T315I), and ABL1(Y253F) are P3049, PV3864, PV3865, PV3866, and PV3863 are full-length human recombinant protein expressed in insect cells and histidine-tagged. Inhibition activities of inhibitors against Abl1 and its mutants are performed in 384-well plates using the FRET-based Z′-Lyte assay system. Briefly, the kinase substrate is diluted into 5 μL of kinase reaction buffer; and the kinase is added. Compounds (10 nL) with indicated concentrations are then delivered to the reaction by using Echo liquid handler, and the mixture is incubated for 30 min at room temperature. Then 5 μL of 2X ATP solution is added to initiate the reaction, and the mixture is further incubated for 2 h at room temperature. The resulting reactions contains 10 μM (for wild-type Abl1, and mutants Y253F, Q252H, M351T, and H396P) or 5 μM (for mutants E255K, G250E, T315I) of ATP, 2 μM of Tyr2 Peptide substrate in 50 mM HEPES (PH 7.5), 0.01% BRIJ-35, 10 mM MgCl2, 1 mM EGTA, 0.0247 μg/mL Abl1, and inhibitors as appropriate. Then, 5 μL of development reagent is added, and the mixture is incubated for 2 h at room temperature before 5 μL of stop solution is added. Fluorescence signal ratio of 445 nm (Coumarin)/520 nm (fluorescin) is examined on an EnVision Multilabel Reader. The data are analyzed using Graphpad Prism5. The data are the mean value of three experiments. |
分子量 | 444.53 |
分子式 | C25H28N6O2 |
CAS No. | 945755-56-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 13 mg/mL (29.2 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2496 mL | 11.2478 mL | 22.4957 mL | 56.2392 mL |
5 mM | 0.4499 mL | 2.2496 mL | 4.4991 mL | 11.2478 mL | |
10 mM | 0.225 mL | 1.1248 mL | 2.2496 mL | 5.6239 mL | |
20 mM | 0.1125 mL | 0.5624 mL | 1.1248 mL | 2.812 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。
XL019 945755-56-6 Angiogenesis Apoptosis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors FLT JAK PDGFR Janus kinase antitumor,HEL.92.1.7 Inhibitor cells XL 019 XL-019 inhibit selective oral phosphorylation tumor inhibitor