A covalent FGFR2 inhibitor
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Lirafugratinib

Item No. 40940

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[4-amino-5-[3-fluoro-4-[(4-methyl-2-pyrimidinyl)oxy]phenyl]-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-2-methyl-2-propenamide
CAS Number
2549174-42-5
Synonyms
  • RLY-4008
Molecular Formula
C28H24FN7O2
Formula Weight
509.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C(C(C)=C)NC1=CC=C(C2=C(C3=C(N)N=CN=C3N2C)C4=CC(F)=C(OC5=NC=CC(C)=N5)C=C4)C=C1
InChi Code
InChI=1S/C28H24FN7O2/c1-15(2)27(37)35-19-8-5-17(6-9-19)24-22(23-25(30)32-14-33-26(23)36(24)4)18-7-10-21(20(29)13-18)38-28-31-12-11-16(3)34-28/h5-14H,1H2,2-4H3,(H,35,37)(H2,30,32,33)
InChi Key
XOQVZSSDIQQUGO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $39

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    5 mg

    $183

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    10 mg

    $347

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    25 mg

    $770

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    Product Description

    Lirafugratinib is a covalent inhibitor of FGFR2 (IC50 = 0.003 µM).1 It is selective for FGFR2 over FGFR1, -3, and -4 (IC50s = 0.77, 0.26, and 15 µM, respectively). Lirafugratinib inhibits the proliferation of SNU-16 gastric cancer cells (IC50 = 0.002 µM). In vivo, lirafugratinib (10 mg/kg) reduces intratumoral FGFR2 phosphorylation and tumor volume in an FGFR2-amplified SNU-16 gastric cancer mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schönherr, H., Ayaz, P., Taylor, A.M., et al. Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2. Proc. Nat. Acad. Sci. USA 121(6), e2317756121 (2024).