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Lirafugratinib

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].

Product Specifications

CAS Number

[2549174-42-5]

Product Name Alternative

RLY-4008

UNSPSC

12352005

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.html

Concentration

10mM

Purity

99.67

Solubility

DMSO : 62.5 mg/mL (ultrasonic; warming; heat to 60°C)

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

Molecular Formula

C28H24FN7O2

Molecular Weight

509.53

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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Available Sizes

Curated Selection

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