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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
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 223 In Stock
5MG 202 In Stock
10MG 297 In Stock
25MG 630 In Stock
50MG 918 In Stock
100MG 1237 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
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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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