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Lirafugratinib

CAT: 0804-HY-147250-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-147250-01Size:5 mg
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Description
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].
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

Chemical Information

Lirafugratinib

Lirafugratinib is an orally bioavailable inhibitor of the fibroblast growth factor receptor 2 (FGFR2), with potential antineoplastic activity. Upon oral administration, lirafugratinib binds to and inhibits FGFR2, which results in the inhibition of FGFR2-mediated signal transduction pathways. This inhibits the proliferation of FGFR2-overexpressing tumor cells. FGFR2, a receptor tyrosine kinase upregulated in many tumor cell types, plays a key role in cellular proliferation, migration and survival.

CAS Number2549174-42-5
PubChem CID155309155
IUPAC NameN-[4-[4-amino-5-[3-fluoro-4-(4-methylpyrimidin-2-yl)oxyphenyl]-7-methylpyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-2-methylprop-2-enamide
Molecular FormulaC28H24FN7O2
Molecular Weight509.5
XLogP4.3
Topological Polar Surface Area121
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count8
Rotatable Bond Count6
Heavy Atom Count38
Formal Charge0
Complexity840
SMILES
CC1=NC(=NC=C1)OC2=C(C=C(C=C2)C3=C(N(C4=NC=NC(=C34)N)C)C5=CC=C(C=C5)NC(=O)C(=C)C)F
InChI
InChI=1S/C28H24FN7O2/c1-15(2)27(37)35-19-8-5-17(6-9-19)24-22(23-25(30)32-14-33-26(23)36(24)4)18-7-10-21(20(29)13-18)38-28-31-12-11-16(3)34-28/h5-14H,1H2,2-4H3,(H,35,37)(H2,30,32,33)
InChIKey
XOQVZSSDIQQUGO-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of Lirafugratinib
CAS: 2549174-42-5
CID: 155309155
Formula: C28H24FN7O2
MW: 509.5
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight509.5
XLogP34.3
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count8
Rotatable Bond Count6
Exact Mass509.19755120
Monoisotopic Mass509.19755120
Topological Polar Surface Area121 Ų
Heavy Atom Count38
Formal Charge0
Complexity840
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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A24163-100Lirafugratinib (RLY-4008) 100mg
A24163-10Lirafugratinib (RLY-4008) 10mg

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