FIIN-3 - EGFR 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEFIIN-3Cat. No.: HY-18603CAS No.: 1637735-84-2分式: CHClNO分量: 691.61作靶点: EGFR; FGFR作通路: JAK/STAT Signaling; 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 : 10 mg/mL

2、(14.46 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.4459 mL 7.2295 mL 14.4590 mL5 mM 0.2892 mL 1.4459 mL 2.8918 mL10 mM 0.1446 mL 0.7230 mL 1.4459 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-3是FGFR 的不可逆抑制剂，对FGFR1，FGFR2，FGFR3和FGFR4

3、的IC50 值分别为13.1，21，31.4和35.3nM。IC50 & Target FGFR1 FGFR2 FGFR3 FGFR413.1 nM (IC50) 21 nM (IC50) 31.4 nM (IC50) 35.3 nM (IC50)体外研究FIIN-3 potently inhibits both WT FGFRs (EC50 in the 1- to 41-nM range) and the gatekeeper mutant of1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEFGFR2 (EC50 of 64 nM). F

4、IIN-3 also strongly inhibits EGFR, with an EC50 of 43 nM. FIIN-3 shows goodpotency against gatekeeper mutant V564F; FIIN-3 also is potent against the gatekeeper-plus-1 mutantE565K; FIIN-3 also displays antiproliferative activity (with an EC50 of 135 nM) against Ba/F3 cellstransformed by the EGFR vII

5、I fusion protein, which has a WT EGFR kinase domain. FIIN-3 shows evenbetter activity against EGFR mutant L858R (EC50 of 17 nM) and moderate activity, displaying an EC50 of231 nM, against the EGFR mutant L858R/T790M mutant. In WT FGFR2 Ba/F3 cells, FIIN-3 completelyinhibits the FGFR2 autophosphoryla

6、tion on Tyr656/657 at concentrations as low as 3 nM. In FGFR2 V564MBa/F3 cells, FIIN-3 is capable of inhibiting the FGFR2 mutant V564M autophosphorylation with partialinhibition at 100 nM and complete inhibition observed at 300 nM 1.PROTOCOLCell Assay 1 TEL-FGFR2transformed Ba/F3 cells are seeded in

7、 a 96-well plate and are treated with each concentrationof FIIN-3. 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):E4869-77McePdfHeightCaution: Product has not been fully validated for medical applications.For rese