Lirafugratinib (hydrochloride)

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[1].

Product Specifications

CAS Number

[2688040-45-9]

Product Name Alternative

RLY-4008 (hydrochloride)

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

FGFR

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/lirafugratinib-hydrochloride.html

Purity

98.96

Solubility

DMSO : 125 mg/mL (ultrasonic)

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

Molecular Formula

C28H25ClFN7O2

Molecular Weight

546.00

Precautions

H302, H315, H319

References & Citations

[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.