Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Erdafitinib (JNJ-42756493) 是一种喹喔啉衍生物,是一种具有口服活性的FGFR 家族抑制剂,抑制FGFR1/2/3/4活性的IC50分别为1.2、 2.5、3.0和5.7 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 248 | 现货 | ||
5 mg | ¥ 578 | 现货 | ||
10 mg | ¥ 822 | 现货 | ||
25 mg | ¥ 1,520 | 现货 | ||
50 mg | ¥ 2,450 | 现货 | ||
100 mg | ¥ 3,490 | 现货 | ||
500 mg | ¥ 7,580 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 683 | 现货 |
产品描述 | Erdafitinib (JNJ-42756493) is a quinoxaline derivative compound, acts on FGFR1/2/3/4. |
靶点活性 | FGFR4:5.7 nM, FGFR3:3.0nM, FGFR1:1.2 nM, FGFR2:2.5nM |
体外活性 | JNJ-42756493 is a potent, oral pan-FGFR tyrosine kinase inhibitor with half-maximal inhibitory concentration values in the low nanomolar range for all members of the FGFR family (FGFR1 to FGFR4), with minimal activity on vascular endothelial growth factor receptor (VEGFR) kinases compared with FGFR kinases (approximately 20-fold potency difference). In vitro, the proliferation of cells treated with JNJ-42756493 is decreased, associated with increased apoptotic death and decreased cell survival[2]. |
体内活性 | In vivo, growth of NCI-H716 tumors is delayed by 5 days by drug treatment alone, although when drug delivery is stopped the relative tumor volume increased compared to control[2]. JNJ-42756493 shows favorable drug like properties and displays a high distribution to lung, liver and kidney tissue. JNJ-42756493 is well tolerated at efficacious doses and results in potent dose-dependent antitumor activity accompanied by pharmacodynamic modulation of tumor FGFR and downstream pathway components[1]. |
细胞实验 | The effect of varying drug concentrations on cell growth and survival is evaluated at 72 h using sulforhodamine B (SRB) assay for the adherent cells (HCT116, HCA7, Caco2) and trypan blue dye exclusion for the suspension cells, NCI-H716. (Only for Reference) |
别名 | 厄达替尼, JNJ-42756493 |
分子量 | 446.54 |
分子式 | C25H30N6O2 |
CAS No. | 1346242-81-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 15 mg/mL(33.6 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 82 mg/mL (183.6 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.2394 mL | 11.1972 mL | 22.3944 mL | 55.986 mL |
5 mM | 0.4479 mL | 2.2394 mL | 4.4789 mL | 11.1972 mL | |
10 mM | 0.2239 mL | 1.1197 mL | 2.2394 mL | 5.5986 mL | |
20 mM | 0.112 mL | 0.5599 mL | 1.1197 mL | 2.7993 mL | |
DMSO | 50 mM | 0.0448 mL | 0.2239 mL | 0.4479 mL | 1.1197 mL |
100 mM | 0.0224 mL | 0.112 mL | 0.2239 mL | 0.5599 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。
Erdafitinib 1346242-81-6 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors FGFR inhibit Fibroblast growth factor receptor 厄达替尼 JNJ42756493 Inhibitor JNJ-42756493 JNJ 42756493 inhibitor