| Identification | Back Directory | [Name]
2-Propenamide, 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- | [CAS]
2549174-42-5 | [Synonyms]
RLY-4008
FGFR2IN3
FGFR2-IN-3
2-Propenamide, 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- | [Molecular Formula]
C28H24FN7O2 | [MOL File]
2549174-42-5.mol | [Molecular Weight]
509.55 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 62.5 mg/mL (122.66 mM; ultrasonic and warming and heat to 60°C) | [form ]
Solid | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
Lirafugratinib (RLY-4008; 1-30 mg/kg; orally, twice daily; 15-30 days) demonstrates antitumor activity in FGFR2-altered cancer xenograft models[1].
| 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[1] | | 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.
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| [IC 50]
FGFR2: 3 nM (IC50) | [References]
[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. DOI:10.1158/2159-8290.CD-23-0475 |
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