FIIN-3

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WARNING: This product is for research use only, not for human or veterinary use.

Description:FIIN-3 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor. FIIN-3 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-3 has the unprecedented ability to inhibit both the EGF receptor (EGFR) and FGFR covalently by targeting two distinct cysteine residues. FIIN-3 bound with FGFR4 V550L and EGFR L858R.

Price and Availability

FIIN-3, purity > 98%, is in stock. Minimum 50mg 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#: 406653Name: FIIN-3CAS#: 1637735-84-2Chemical Formula: C34H36Cl2N8O4Exact Mass: 690.22366Molecular Weight: 691.60684Elemental Analysis: C, 59.05; H, 5.25; Cl, 10.25; N, 16.20; O, 9.25

Synonym:FIIN3; FIIN 3; FIIN-3.

IUPAC/Chemical Name:N-(4-((3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)ureido)methyl)phenyl)acrylamide

InChi Key:SFLKJNSBBVSPFE-UHFFFAOYSA-N

InChi Code:InChI=1S/C34H36Cl2N8O4/c1-5-30(45)40-24-8-6-22(7-9-24)20-44(34(46)41-33-31(35)26(47-3)18-27(48-4)32(33)36)29-19-28(37-21-38-29)39-23-10-12-25(13-11-23)43-16-14-42(2)15-17-43/h5-13,18-19,21H,1,14-17,20H2,2-4H3,(H,40,45)(H,41,46)(H,37,38,39)

SMILES Code:O=C(NC1=CC=C(C=C1)CN(C(NC2=C(C(OC)=CC(OC)=C2Cl)Cl)=O)C3=CC(NC4=CC=C(C=C4)N5CCN(CC5)C)=NC=N3)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.