Cat. No.: HY-147250

Lirafugratinib

(Synonyms: RLY-4008)

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

Purity: 99.62%
CAS No.: 2549174-42-5
Formula: C₂₈H₂₄FN₇O₂
Molecular Weight:509.53

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Lirafugratinib Chemical Structure

CAS No.: 2549174-42-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

FGFR2

3 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	>1000 nM Compound: 6	Antiproliferation activity against mouse BaF3 cells expressing FGFR1 incubated for 72 hrs by CCK8 assay Antiproliferation activity against mouse BaF3 cells expressing FGFR1 incubated for 72 hrs by CCK8 assay	[PMID: 38718625]
BaF3	IC₅₀	>1000 nM Compound: 6	Antiproliferation activity against mouse BaF3 cells incubated for 72 hrs by CCK8 assay Antiproliferation activity against mouse BaF3 cells incubated for 72 hrs by CCK8 assay	[PMID: 38718625]
BaF3	IC₅₀	8.9 nM Compound: 6	Antiproliferation activity against mouse BaF3 cells expressing FGFR2 incubated for 72 hrs by CCK8 assay Antiproliferation activity against mouse BaF3 cells expressing FGFR2 incubated for 72 hrs by CCK8 assay	[PMID: 38718625]

In Vitro

Lirafugratinib (RLY-4008) 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) induces dose-dependent cleavage of caspase-3 and poly (ADP-ribose) polymerase (PARP)-early markers of apoptosis^[1].
Lirafugratinib (2h) 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.

Apoptosis Analysis^[1]

Cell Line:

FGFR2-amplified gastric cancer cell line SNU-16
Concentration:

IC50 (6 nM), IC90
Incubation Time:

24 h
Result:

Induced dose-dependent cleavage of caspase-3 and poly (ADP-ribose) polymerase (PARP)-early markers of apoptosis.

Apoptosis Analysis^[1]

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

Lirafugratinib (RLY-4008; 1-30 mg/kg; orally, twice daily; 15-30 days) demonstrates antitumor activity in FGFR2-altered cancer xenograft models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female BALB/c nude mice with SNU-16 and AN3CA xenografts; female NOD SCID mice with CC13-7 and ICC13-7-FGFR2^V564F 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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2549174-42-5
Appearance Solid
Molecular Weight 509.53
Formula C₂₈H₂₄FN₇O₂
Color Off-white to light yellow
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
Synonyms

RLY-4008
Shipping

Room temperature in continental US; may vary elsewhere.

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

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

In Vitro:

DMSO : 62.5 mg/mL (122.66 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9626 mL

9.8130 mL

19.6259 mL

5 mM

0.3925 mL

1.9626 mL

3.9252 mL

10 mM

0.1963 mL

0.9813 mL

1.9626 mL

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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	1.9626 mL	9.8130 mL	19.6259 mL	49.0648 mL
	5 mM	0.3925 mL	1.9626 mL	3.9252 mL	9.8130 mL
	10 mM	0.1963 mL	0.9813 mL	1.9626 mL	4.9065 mL
	15 mM	0.1308 mL	0.6542 mL	1.3084 mL	3.2710 mL
	20 mM	0.0981 mL	0.4906 mL	0.9813 mL	2.4532 mL
	25 mM	0.0785 mL	0.3925 mL	0.7850 mL	1.9626 mL
	30 mM	0.0654 mL	0.3271 mL	0.6542 mL	1.6355 mL
	40 mM	0.0491 mL	0.2453 mL	0.4906 mL	1.2266 mL
	50 mM	0.0393 mL	0.1963 mL	0.3925 mL	0.9813 mL
	60 mM	0.0327 mL	0.1635 mL	0.3271 mL	0.8177 mL
	80 mM	0.0245 mL	0.1227 mL	0.2453 mL	0.6133 mL
	100 mM	0.0196 mL	0.0981 mL	0.1963 mL	0.4906 mL

Keywords

Lirafugratinib

1 Cited Publications

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Lirafugratinib

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Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Lirafugratinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Lirafugratinib

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Lirafugratinib Related Classifications

HY-147250 Related Classifications