Powder: -20°C for 3 years | In solvent: -80°C for 1 year
(E/Z)-Zotiraciclib ((E/Z)-TG02) 是一种 CDK2、JAK2和FLT3的抑制剂,IC50分别为 13、73 和 56 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 292 | 现货 | ||
2 mg | ¥ 413 | 现货 | ||
5 mg | ¥ 663 | 现货 | ||
10 mg | ¥ 980 | 现货 | ||
25 mg | ¥ 1,780 | 现货 | ||
50 mg | ¥ 2,980 | 现货 | ||
100 mg | ¥ 4,390 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 728 | 现货 |
产品描述 | (E/Z)-Zotiraciclib ((E/Z)-TG02) inhibits CDK2, JAK2, and FLT3 effectively with IC50s of 13, 73, and 56 nM, respectively. |
靶点活性 | JAK2:73 nM, FLT3:56 nM, CDK2:13 nM |
体外活性 | (E/Z)-Zotiraciclib has a highly novel kinase inhibitory spectrum inhibiting 17 kinases from a panel of 63, 11 of which are CDK/JAK/FLT family members. Human CYP1A2, 3A4, 2C9, and 2C19 isoforms are not inhibited by (E/Z)-Zotiraciclib at the highest tested concentration of 25 μM, but (E/Z)-Zotiraciclib inhibits CYP2D6 with an IC50 of 0.95 μM, approximately at the plasma Cmax?observed at the maximum tolerated dose. (E/Z)-Zotiraciclib inhibits cell proliferation concentrations in HCT-116 with an IC50 of 0.079 μM and HL-60 with an IC50 of 0.059 μM[1]. (E/Z)-Zotiraciclib is a novel small molecule potent CDK/JAK2/FLT3 inhibitor and mainly metabolized by CYP3A4 and CY1A2 in vitro[2]. |
体内活性 | Treatment with (E/Z)-Zotiraciclib (75 mg/kg p.o. q.d. 3×/week) significantly inhibits the growth of tumors with a mean TGI of 82%, while the lower dose(50 mg/kg p.o. 3×/week) is marginally effective. Treatment with (E/Z)-Zotiraciclib using either regime significantly inhibits the growth of tumors with mean TGIs of 42% and 63% for the oral and ip delivery methods, respectively[1]. In pharmacokinetic studies, (E/Z)-Zotiraciclib shows moderate to high systemic clearance (relative to liver blood flow), high volume of distribution (>0.6 L/kg), the oral bioavailability of 24%, ~4 and 37% in mice, rats, and dogs, respectively; and extensive tissue distribution in mice[2]. |
别名 | (E/Z)-TG02, (E/Z)-SB1317 |
分子量 | 372.46 |
分子式 | C23H24N4O |
CAS No. | 937270-47-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 40mg/mL (107.39mM)
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 | |
20 mM | 0.1342 mL | 0.6712 mL | 1.3424 mL | 3.3561 mL | |
50 mM | 0.0537 mL | 0.2685 mL | 0.537 mL | 1.3424 mL | |
100 mM | 0.0268 mL | 0.1342 mL | 0.2685 mL | 0.6712 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。
(E/Z)-Zotiraciclib 937270-47-8 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors JAK CDK FLT multiple myeloma JAK2 Fms like tyrosine kinase 3 (E/Z)-TG02 Cyclin dependent kinase (E/Z)-SB1317 FLT3 (E/Z)-SB 1317 Janus kinase CD135 leukemias Inhibitor (E/Z)-SB-1317 CDK2 Cluster of differentiation antigen 135 inhibit cancer (E/Z) Zotiraciclib (E/Z)Zotiraciclib inhibitor