Art. -Nr.: HY-147250A

Lirafugratinib hydrochloride

(Synonyms: RLY-4008 hydrochloride)

1 Cited Publications

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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.

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Reinheit: 98.96%
CAS. Nr.: 2688040-45-9
Formel: C₂₈H₂₅ClFN₇O₂
Molecular Weight:546.00

Speicherung:

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

Lirafugratinib hydrochloride Chemical Structure

CAS. Nr.: 2688040-45-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

FGFR2

3 nM (IC₅₀)

In Vitro

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.

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) hydrochloride 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.

Chemical Information

CAS. Nr. 2688040-45-9
Appearance Solid
Molecular Weight 546.00
Formel C₂₈H₂₅ClFN₇O₂
Color Light brown to brown
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
Synonyms

RLY-4008 hydrochloride
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8315 mL

9.1575 mL

18.3150 mL

5 mM

0.3663 mL

1.8315 mL

3.6630 mL

10 mM

0.1832 mL

0.9158 mL

1.8315 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
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)

Verweise

[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	1.8315 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

Keywords

Lirafugratinib hydrochloride

1 Cited Publications

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Lirafugratinib hydrochloride

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Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

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Publications Citing Use of MedChemExpress (MCE) Lirafugratinib hydrochloride

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lirafugratinib hydrochloride

Bioactive Compound Library Max

Bioactive Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer 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

MCE Bioactive Compound Library

Covalent Screening Library Plus

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 hydrochloride

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lirafugratinib hydrochloride Related Classifications

HY-147250A Related Classifications