FIIN-2newfeatured
WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#:406652
CAS#:1633044-56-0
Description:FIIN-2 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor. FIIN-2 is the first inhibitor that can potently inhibit the proliferation of cells dependent upon the gatekeeper mutants of FGFR1 or FGFR2, which confer resistance to first-generation clinical FGFR inhibitors such as NVP-BGJ398 and AZD4547. FIIN-2 also binds in the DFG-out mode despite lacking a functional group necessary to occupy the pocket vacated upon the DFG-out flip.
Price and Availability
FIIN-2, purity > 98%, is in stock. Minimum 100mg order required. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.
Chemical Structure
Theoretical Analysis
MedKoo Cat#: 406652Name: FIIN-2CAS#: 1633044-56-0Chemical Formula: C35H38N8O4Exact Mass: 634.3016Molecular Weight: 634.72742Elemental Analysis: C, 66.23; H, 6.03; N, 17.65; O, 10.08
Synonym:FIIN2; FIIN 2; FIIN-2.
IUPAC/Chemical Name:N-(4-((3-(3,5-dimethoxyphenyl)-7-((4-(4-methylpiperazin-1-yl)phenyl)amino)-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl)methyl)phenyl)acrylamide
InChi Key:DVBPRWJMHURKHP-UHFFFAOYSA-N
InChi Code:InChI=1S/C35H38N8O4/c1-5-32(44)37-26-8-6-24(7-9-26)22-43-33-25(23-42(35(43)45)29-18-30(46-3)20-31(19-29)47-4)21-36-34(39-33)38-27-10-12-28(13-11-27)41-16-14-40(2)15-17-41/h5-13,18-21H,1,14-17,22-23H2,2-4H3,(H,37,44)(H,36,38,39)
SMILES Code:O=C(NC1=CC=C(C=C1)CN2C(N(CC3=CN=C(N=C32)NC4=CC=C(C=C4)N5CCN(CC5)C)C6=CC(OC)=CC(OC)=C6)=O)C=C
Technical Data
Additional Information
References
1: Tan L, Wang J, Tanizaki J, Huang Z, Aref AR, RusanM, Zhu SJ, Zhang Y, Ercan D, Liao RG, Capelletti M, Zhou W, Hur W, Kim N, Sim T, Gaudet S, BarbieDA, Yeh JR, Yun CH, Hammerman PS, Mohammadi M, Jänne PA, Gray NS. Development ofcovalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):E4869-77. doi: 10.1073/pnas.1403438111. Epub 2014 Oct 27. PubMed PMID: 25349422; PubMedCentralPMCID: PMC4234547.
2: Huang Z, Tan L, Wang H, Liu Y, Blais S, Deng J, Neubert TA, Gray NS,Li X, Mohammadi M. DFG-out mode of inhibition by an irreversible type-1inhibitor capable of overcoming gate-keeper mutations in FGF receptors. ACS ChemBiol. 2015 Jan 16;10(1):299-309. doi: 10.1021/cb500674s. Epub 2014 Oct 27. PubMedPMID: 25317566; PubMed Central PMCID: PMC4301177.
