Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TG101209 是一种选择性有效的 JAK2抑制剂,IC50值为 6 nM。它能抑制 Flt3和RET 的活性,IC50值分别为 25 nM 和 17 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 348 | 现货 | ||
5 mg | ¥ 583 | 现货 | ||
10 mg | ¥ 995 | 现货 | ||
50 mg | ¥ 2,263 | 现货 | ||
100 mg | ¥ 3,996 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 652 | 现货 |
产品描述 | TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM. |
靶点活性 | JAK2:6 nM |
体外活性 | 与安慰剂处理的动物相比,TG101209处理的动物体内循环肿瘤细胞负荷显著减少,呈剂量依赖性,在+11天时减少比例达到20%.100 mg/kg TG101209有效延长JAK2V617F诱发的患病动物的存活时间(10天). |
体内活性 | TG101209抑制HCC2429和H460肺癌细胞中存活素,并降低STAT3的磷酸化作用。TG101209在表达人JAK2V617F的急性髓细胞性白血病细胞系中,诱导细胞周期阻滞和细胞凋亡,并抑制JAK2V617F,STAT5和STAT3的磷酸化。TG101209抑制表达JAK2V617F或MPLW515L突变体的Ba/F3细胞生长,IC50为B200 nM。TG101209抑制来自携带JAK2V617F或MPL515突变的原始祖细胞的造血集落的生长。TG101209明显减少STAT5磷酸化,而不影响STAT5蛋白质的总量。TG101209消除BCR-JAK2和STAT5的磷酸化,减少Bcl-xL表达,并引发转化的Ba/F3细胞凋亡。 |
激酶实验 | Cell-free Kinase Activity Assays: IC50 values for TG101209 are determined using a luminescence-based kinase assay with recombinant JAK2, VEGFR2/KDR, and JAK3 obtained from Upstate Cell Signaling Solutions. Kinase reactions are carried out in a buffer consisting of 40 mM Tris buffer (pH 7.4), 50 mM MgCl2, 800?M EGTA, 350?M Triton X-100, 2?M ?-mercaptoethanol, 100?M peptide substrate, and an appropriate amount of JAK2, VEGFR2/KDR or JAK3 such that the assay is linear over 60 minutes. The reaction is initiated by the addition of 10?L of ATP to a final concentration of 3 mM and terminated by the addition of Kinase-Glo reagent after 60 minutes. Luciferase activity is quantified using an Ultra 384 instrument set for luminosity measurements. IC50 values are derived from experimental data using the non-linear curve fitting capabilities of the GraphPad Prism 4.0 software. The single concentration inhibition data for a panel of 63 kinases is determined using the SelectScreen TM service. |
细胞实验 | In brief, approximately 2 × 103 cells are plated into microtiterplate wells in 100 ml RPMI-1640 growth media with indicated concentrations of TG101209. The relative growth of cells is quantified at 24-hour intervals using Cell Proliferation Kit II (XTT) as per manufacturer's guidelines. After incubation, 20 mL of XTT is added to the wells and allowed to incubate for 4-6 hours. The colored formazan product is measured spectrophotometrically at 450 nm with correction at 650 nm, and IC50 values are determined using the GraphPad Prism 4.0 software. Data are subjected to a non-linear regression-fit analysis and IC50 values are determined as the concentration that inhibited proliferation by 50%. All experiments are done in triplicate and the results normalized to growth of untreated cells.(Only for Reference) |
分子量 | 509.67 |
分子式 | C26H35N7O2S |
CAS No. | 936091-14-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 94 mg/mL (184.4 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 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 | 1.9621 mL | 9.8103 mL | 19.6205 mL | 49.0513 mL |
5 mM | 0.3924 mL | 1.9621 mL | 3.9241 mL | 9.8103 mL | |
10 mM | 0.1962 mL | 0.981 mL | 1.9621 mL | 4.9051 mL | |
20 mM | 0.0981 mL | 0.4905 mL | 0.981 mL | 2.4526 mL | |
50 mM | 0.0392 mL | 0.1962 mL | 0.3924 mL | 0.981 mL | |
100 mM | 0.0196 mL | 0.0981 mL | 0.1962 mL | 0.4905 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。
TG101209 936091-14-4 Angiogenesis Apoptosis Autophagy Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors FLT c-RET JAK Cluster of differentiation antigen 135 RET Inhibitor Janus kinase TG-101209 CD135 Fms like tyrosine kinase 3 FLT3 TG 101209 inhibit inhibitor