厄达替尼 T3726

Product Introduction
Bioactivity


英文名: Erdafitinib

描述: 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。

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)

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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 15 mg/mL(33.6 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 5.63 mg/mL (12.6 mM)


关键字: inhibit | Apoptosis | Fibroblast growth factor receptor | FGFR | JNJ42756493 | Inhibitor | JNJ 42756493 | Erdafitinib

相关产品: Hexamethonium Bromide | BIX02188 | Isoliquiritigenin | Isatin | Demethoxycurcumin | EB-3D | Diclofenac | Toyocamycin | Agrimonolide | Taurochenodeoxycholic acid sodium

相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library

厄达替尼 T3726信息由TargetMol中国为您提供，如您想了解更多关于厄达替尼 T3726报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途