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FIIN-2

CAS No. 1633044-56-0

FIIN-2( FIIN2 | FIIN 2 | FIIN-2 )

Catalog No. M17351 CAS No. 1633044-56-0

FIIN-2, an irreversible, pan-FGFR inhibitor, inhibits FGFR1/2/3/4 with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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1 mL x 10 mM in DMSO 86 In Stock
2MG 46 In Stock
5MG 61 In Stock
10MG 93 In Stock
25MG 198 In Stock
50MG 295 In Stock
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Biological Information

  • Product Name
    FIIN-2
  • Note
    Research use only, not for human use.
  • Brief Description
    FIIN-2, an irreversible, pan-FGFR inhibitor, inhibits FGFR1/2/3/4 with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM, respectively.
  • 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.
  • In Vitro
    FIIN-2 potently inhibits WT FGFRs (EC50s in the 1- to 93-nM range) and the gatekeeper mutant of FGFR2 (EC50 of 58 nM). FIIN-2 also moderately inhibits EGFR, with an IC50 of 204 nM. FIIN-2 inhibits proliferation of FGFR1-4 Ba/F3 cells with EC50s in the single- to double-digit nanomolar range and are especially potent against FGFR2, with EC50s in the 1-nM range. FIIN-2 shows good potency against gatekeeper mutant V564F.
  • In Vivo
    Treatment of fish in the embryonic state with either FIIN-2 causes defects to the posterior mesoderm similar to the phenotypes reported following genetic knockdown of FGFR or treatment with other reported FGFR inhibitors. FIIN-2 causes mild or severe phenotypes to the tail morphogenesis in all treated embryonic zebrafish.
  • Synonyms
    FIIN2 | FIIN 2 | FIIN-2
  • Pathway
    GPCR/G Protein
  • Target
    Dopamine Receptor
  • Recptor
    FGFR1| FGFR2| FGFR3| FGFR4
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    1633044-56-0
  • Formula Weight
    634.73
  • Molecular Formula
    C35H38N8O4
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : ≥ 30 mg/mL 47.26 mM
  • SMILES
    CN1CCN(CC1)c1ccc(cc1)Nc1ncc2CN(C(=O)N(c2n1)Cc1ccc(cc1)NC(=O)C=C)c1cc(cc(c1)OC)OC
  • 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

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Tan L, et al. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):E4869-4877.
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