2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. Lirafugratinib hydrochloride

Lirafugratinib hydrochloride  (Synonyms: RLY-4008 hydrochloride)

Cat. No.: HY-147250A Purity: 98.73%
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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.

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

Lirafugratinib hydrochloride Chemical Structure

Lirafugratinib hydrochloride Chemical Structure

CAS No. : 2688040-45-9

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Lirafugratinib hydrochloride Related Antibodies

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

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Description

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].

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.

Lirafugratinib hydrochloride Related Antibodies

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-FGFR2V564F 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.
Molecular Weight

546.00

Formula

C28H25ClFN7O2
CAS No.
Appearance

Solid

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
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
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8315 mL 9.1575 mL 18.3150 mL
5 mM 0.3663 mL 1.8315 mL 3.6630 mL
View the Complete Stock Solution Preparation Table

* 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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Lirafugratinib hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lirafugratinib2688040-45-9RLY-4008RLY4008RLY 4008FGFRFibroblast growth factor receptororallyirreversiblecovalentlyCys491PARPInhibitorinhibitorinhibit

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