Lirafugratinib hydrochloride
Based on 1 publication(s) in Google Scholar
Lirafugratinib (RLY-4008) hydrochloride is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib hydrochloride covalently binds to Cys491. Lirafugratinib hydrochloride targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs.
For research use only. We do not sell to patients.
- Purity: 98.96%
- CAS No.: 2688040-45-9
- Formula: C28H25ClFN7O2
- Molecular Weight:546.00
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Lirafugratinib hydrochloride
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Biological Activity
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FGFR2 3 nM (IC50) |
Lirafugratinib (RLY-4008) hydrochloride has >250-fold selectivity over FGFR1, and >80- and >5,000-fold selectivity over FGFR3 and FGFR4, respectively. The reversible binding of Lirafugratinib promotes a rigid and extended P-loop in FGFR1 that disfavors covalent bond formation while minimally affecting the conformation of the P-loop in FGFR2, enabling efficient covalent bond formation and leading to FGFR2 selectivity[1].
Lirafugratinib (24h) hydrochloride induces dose-dependent cleavage of caspase-3 and poly (ADP-ribose) polymerase (PARP)-early markers of apoptosis[1].
Lirafugratinib (2h) hydrochloride demonstrates a dose-dependent reduction of phosphorylation of FGFR2 signaling pathway nodes, including FRS2, AKT, and ERK[1].
RLY-4008 inhibits cellular proliferation with IC50<14 nM in FGFR2-dependent cell lines including KATO III, SNU-16 and NCI-H716, ICC13-7, and MFE-296, FGFR2N549K and AN3CA, FGFR2K310R; N549K and JHUEM-2, FGFR2C383R[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:FGFR2-amplified gastric cancer cell line SNU-16
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Concentration:IC50 (6 nM), IC90
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Incubation Time:24 h
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Result:Induced dose-dependent cleavage of caspase-3 and poly (ADP-ribose) polymerase (PARP)-early markers of apoptosis.
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Cell Line:FGFR2-amplified gastric cancer cell line SNU-16
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Concentration:IC50 (6 nM), IC90
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Incubation Time:2 h
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Result:Demonstrated a dose-dependent reduction of phosphorylation of FGFR2 signaling pathway nodes, including FRS2, AKT, and ERK.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:1, 3, 10, 30 mg/kg
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Administration:Orally; twice daily; for 15-30 days
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Result:Exhibited dose-dependent antitumor activity and induced tumor regression in all models.
Chemical Information
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CAS No. 2688040-45-9
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Appearance Solid
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Molecular Weight 546.00
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Formula C28H25ClFN7O2
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Color Light brown to brown
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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.Cl
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Synonyms
RLY-4008 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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PLoS One
The FGFR inhibitor pemigatinib overcomes cancer drug resistance to KRAS G12C inhibitors in mesenchymal lung cancer. [Abstract]2025 Aug 11;20(8):e0327588. PMID: 40788860
Solvent & Solubility
DMSO : 125 mg/mL (228.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8315 mL | 9.1575 mL | 18.3150 mL | 45.7875 mL |
| 5 mM | 0.3663 mL | 1.8315 mL | 3.6630 mL | 9.1575 mL | |
| 10 mM | 0.1832 mL | 0.9158 mL | 1.8315 mL | 4.5788 mL | |
| 15 mM | 0.1221 mL | 0.6105 mL | 1.2210 mL | 3.0525 mL | |
| 20 mM | 0.0916 mL | 0.4579 mL | 0.9158 mL | 2.2894 mL | |
| 25 mM | 0.0733 mL | 0.3663 mL | 0.7326 mL | 1.8315 mL | |
| 30 mM | 0.0611 mL | 0.3053 mL | 0.6105 mL | 1.5263 mL | |
| 40 mM | 0.0458 mL | 0.2289 mL | 0.4579 mL | 1.1447 mL | |
| 50 mM | 0.0366 mL | 0.1832 mL | 0.3663 mL | 0.9158 mL | |
| 60 mM | 0.0305 mL | 0.1526 mL | 0.3053 mL | 0.7631 mL | |
| 80 mM | 0.0229 mL | 0.1145 mL | 0.2289 mL | 0.5723 mL | |
| 100 mM | 0.0183 mL | 0.0916 mL | 0.1832 mL | 0.4579 mL |
Lirafugratinib hydrochloride Related Classifications
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