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FGFR2-IN-3

CAS No. 2549174-42-5

FGFR2-IN-3( —— )

Catalog No. M35365 CAS No. 2549174-42-5

FGFR2-IN-3 is an orally active selective FGFR2 inhibitor.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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2MG 132 Get Quote
5MG 202 Get Quote
10MG 297 Get Quote
25MG 610 Get Quote
50MG 908 Get Quote
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Biological Information

  • Product Name
    FGFR2-IN-3
  • Note
    Research use only, not for human use.
  • Brief Description
    FGFR2-IN-3 is an orally active selective FGFR2 inhibitor.
  • Description
    Lirafugratinib (RLY-4008) is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib covalently binds to Cys491. Lirafugratinib targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs.
  • In Vitro
    Apoptosis AnalysisCell Line:FGFR2-amplified gastric cancer cell line SNU-16 Concentration:IC50 (6 nM), IC90 Incubation Time:24 hResult:Induced dose-dependent cleavage of caspase-3 and poly (ADP-ribose) polymerase (PARP)-early markers of apoptosis.Apoptosis Analysis Cell Line:FGFR2-amplified gastric cancer cell line SNU-16 Concentration:IC50 (6 nM), IC90 Incubation Time:2 h Result:Demonstrated a dose-dependent reduction of phosphorylation of FGFR2 signaling pathway nodes, including FRS2, AKT, and ERK.
  • In Vivo
    Animal Model:Female BALB/c nude mice with SNU-16 and AN3CA xenografts; female NOD SCID mice with CC13-7 and ICC13-7-FGFR2V564F xenografts Dosage:1, 3, 10, 30 mg/kg Administration:Orally; twice daily; for 15-30 days Result:Exhibited dose-dependent antitumor activity and induced tumor regression in all models.
  • Synonyms
    ——
  • Pathway
    Angiogenesis
  • Target
    FGFR
  • Recptor
    FGFR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2549174-42-5
  • Formula Weight
    509.53
  • Molecular Formula
    C28H24FN7O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 62.5 mg/mL (122.66 mM; Ultrasonic (<60°C)
  • SMILES
    CC(=C)C(=O)Nc1ccc(cc1)-c1c(-c2ccc(Oc3nccc(C)n3)c(F)c2)c2c(N)ncnc2n1C
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Vivek Subbiah, et al. RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across FGFR2 Alterations and Resistance Mutations. Cancer Discov. 2023 Sep 6;13(9):2012-2031.?
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