Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SB1317 (TG02) 是一种有效的细胞周期蛋白依赖性激酶 (CDKs)、Janus 激酶 2 (JAK2) 和 Fms 样酪氨酸激酶-3 (FLT3) 抑制剂。 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 SB1317 hydrochloride (1204918-72-8(free base)) 的水溶性和稳定性通常比游离态更好。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 1,981 | 5日内发货 |
SB1317 的其他形式现货产品:
产品描述 | SB1317 (TG02) is a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3). |
体外活性 | SB1317 has a highly novel kinase inhibitory spectrum inhibiting 17 kinases from a panel of 63, 11 of which are CDK/JAK/FLT family members. The others, Lck, Fyn, Fms, TYRO3, ERK5, and p38δ, are implicated in inflammatory and proliferative processes. Human CYP1A2, 3A4, 2C9, and 2C19 isoforms are not inhibited by SB1317 at the highest tested concentration of 25 μM, but SB1317 inhibits CYP2D6 with IC50=0.95 μM, approximately at the plasma Cmax observed at the maximum tolerated dose. SB1317 inhibits cell proliferation concentrations in HCT-116 (IC50=0.079 μM) and HL-60 (IC50=0.059 μM)[1]. SB1317 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor. SB1317 is mainly metabolized by CYP3A4 and CY1A2 in vitro. SB1317 does not inhibit any of the major human CYPs in vitro except CYP2D6 (IC50=1 μM). SB1317 does not significantly induce CYP1A and CYP3A4 in human hepatocytes in vitro[2]. |
激酶实验 | The recombinant enzymes (CDK2/cyclin A, JAK2, and FLT3) are used. All assays are carried out in 384-well white microtiter plates using the PKLight assay system. This assay platform is a luminometric assay for the detection of ATP in the reaction using a luciferase-coupled reaction. The compounds are tested at eight concentrations prepared from 3- or 4-fold serial dilution starting at 10 μM. For CDK2/cyclin A assay, the reaction mixture consisted of the following components in 25 μL of assay buffer (50 mM Hepes, pH 7.5, 10 mM MgCl2, 5 mM MnCl2, 5 mM BGP, 1 mM DTT, 0.1 mM sodium orthovanadate), 1.4 μg/mL of CDK2/cyclin A complex, 0.5 μM RbING substrate, and 0.5 μM ATP. The mixture is incubated at room temperature for 2 h. Then 13 μL of PKLight ATP detection reagent is added and the mixture is incubated for 10 min. Luminescence signals are detected on a multilabel plate reader. The analytical software Prism 5.0 is used to generate IC50 values from the data[1]. |
细胞实验 | SB1317 is prepared in DMSO and stored, and then diluted with appropriate medium before use[1]. All cell lines are obtained from the American Type Culture Collection and cultured. For proliferation assays in 96-well plates, 20 000 cells are seeded in 100 μL of medium and treated the following day with compounds (e.g., SB1317 ) (in triplicate) at concentrations up to 10 μM for 48 h. Cell viability is monitored using the CellTiter-96 Aqueous One solution cell proliferation assay. Dose-response curves are plotted to determine IC50 values for the compounds using the XL-fit software[1]. |
别名 | TG02 |
分子量 | 372.46 |
分子式 | C23H24N4O |
CAS No. | 1204918-72-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mM
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6849 mL | 13.4243 mL | 26.8485 mL | 67.1213 mL |
5 mM | 0.537 mL | 2.6849 mL | 5.3697 mL | 13.4243 mL | |
10 mM | 0.2685 mL | 1.3424 mL | 2.6849 mL | 6.7121 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。
SB1317 1204918-72-8 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors FLT JAK CDK TG 02 SB 1317 TG02 TG-02 SB-1317 Inhibitor inhibitor inhibit