Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PRN1371 是一种高效的、选择性的FGFR1-4和CSF1R 抑制剂,对FGFR1,FGFR2,FGFR3,FGFR4 和 CSF1R 的IC50值分别为 0.6,1.3,4.1,19.3 和 8.1 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 679 | 现货 | ||
2 mg | ¥ 980 | 现货 | ||
5 mg | ¥ 1,830 | 现货 | ||
10 mg | ¥ 3,230 | 现货 | ||
25 mg | ¥ 5,350 | 现货 | ||
50 mg | ¥ 7,530 | 现货 | ||
100 mg | ¥ 9,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,250 | 现货 |
产品描述 | PRN1371 is a specific and potent FGFR1-4 and CSF1R inhibitor (IC50s: 0.6/1.3/4.1/19.3/8.1 nM for FGFR1/2/3/4 and CSF1R). |
靶点活性 | FGFR2:1.3 nM (IC50), FGFR1:0.6 nM (IC50), CSF1R:8.1 nM (IC50), FGFR3:4.1 nM (IC50), FGFR4:19.3 nM (IC50) |
体外活性 | PRN1371 presents a unique profile of high biochemical and cellular potency (FGFR1 IC50:0.6 nM, SNU16 IC50: 2.6 nM), prolonged target engagement (FGFR1 occupancy 24 h=96%), < 30% hERG inhibition at 1 μM, and good predicted ADME stability with BME reactivity Kd>100 μM. |
体内活性 | In PK studies of rat, dog, and cynomolgus monkey, PRN1371show rapid iv clearance in all species. PRN1371 shows rapid clearance (Cl=160 mL per min per kg), yet dosing p.o (20 mg/kg) demonstrates high oral exposure (AUC=4348 h·ng/mL) and a reasonable half-life (t1/2=3.8 h). Low levels of pFGFR2 confirm the ability of PRN1371 to block FGFR2 activity in tumor tissue. PRN1371 induces a dose-dependent reduction in tumor volume and up to 68% tumor growth inhibition at the highest dose of 10 mg/kg b.i.d. following 27 days of treatment. All doses are well tolerated with no significant bodyweight loss. |
分子量 | 561.46 |
分子式 | C26H30Cl2N6O4 |
CAS No. | 1802929-43-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 12 mg/mL (21.38 mM), sonification/heating is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7811 mL | 8.9054 mL | 17.8107 mL | 44.5268 mL |
5 mM | 0.3562 mL | 1.7811 mL | 3.5621 mL | 8.9054 mL | |
10 mM | 0.1781 mL | 0.8905 mL | 1.7811 mL | 4.4527 mL | |
20 mM | 0.0891 mL | 0.4453 mL | 0.8905 mL | 2.2263 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。
PRN1371 1802929-43-6 Angiogenesis Tyrosine Kinase/Adaptors c-Fms FGFR CSF-1R PRN 1371 inhibit CSF1R Inhibitor colony stimulating factor 1 receptor PRN-1371 CSF-1 receptor Fibroblast growth factor receptor inhibitor