FIIN-2 - FGFR 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEFIIN-2Cat. No.: HY-18602CAS No.: 1633044-56-0分式: CHNO分量: 634.73作靶点: FGFR作通路: Protein Tyrosine Kinase/RTK储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 30 mg/mL (47.26 mM)* means soluble, b

2、ut saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.5755 mL 7.8774 mL 15.7547 mL5 mM 0.3151 mL 1.5755 mL 3.1509 mL10 mM 0.1575 mL 0.7877 mL 1.5755 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 FIIN-2是FGFR 的不可逆抑制剂，对FGFR1，FGFR2，FGFR3和FGFR4的IC50 值分别为3.1，4.3

3、，27和45 nM。IC50 & Target FGFR1 FGFR2 FGFR3 FGFR43.1 nM (IC50) 4.3 nM (IC50) 27 nM (IC50) 45 nM (IC50)体外研究FIIN-2 potently inhibits WT FGFRs (EC50s in the 1- to 93-nM range) and the gatekeeper mutant of FGFR21/2 Master of Small Molecules 您边的抑制剂师www.MedChemE(EC50 of 58 nM). FIIN-2 also moderately inhibi

4、ts EGFR, with an IC50 of 204 nM. FIIN-2 inhibits proliferationof FGFR1-4 Ba/F3 cells with EC50s in the single- to double-digit nanomolar range and are especially potentagainst FGFR2, with EC50s in the 1-nM range. FIIN-2 shows good potency against gatekeeper mutantV564F 1.体内研究 Treatment of fish in th

5、e embryonic state with either FIIN-2 causes defects to the posterior mesoderm similarto the phenotypes reported following genetic knockdown of FGFR or treatment with other reported FGFRinhibitors. FIIN-2 causes mild or severe phenotypes to the tail morphogenesis in all treated embryoniczebrafish 1.P

6、ROTOCOLCell Assay 1 TEL-FGFR2transformed Ba/F3 cells are seeded in a 96-well plate and are treated with each concentrationof the compounds. After 72 h the cells are assessed by MTS tetrazolium assay 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Tan L, et al. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc Natl AcadSci U S A. 2014 Nov 11;111(45):E4869-4877.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use onl