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

Lirafugratinib  (Synonyms: RLY-4008)

Cat. No.: HY-147250 Purity: 99.60%
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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.

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

Lirafugratinib Chemical Structure

Lirafugratinib Chemical Structure

CAS No. : 2549174-42-5

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 286 In-stock
Solution
10 mM * 1 mL in DMSO USD 286 In-stock
Solid
5 mg USD 260 In-stock
10 mg USD 380 In-stock
25 mg USD 800 In-stock
50 mg USD 1280 In-stock
100 mg USD 2100 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Lirafugratinib:

Lirafugratinib Related Antibodies

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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].

IC50 & Target[1]

FGFR2

3 nM (IC50)

In Vitro

Lirafugratinib (RLY-4008) 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) induces dose-dependent cleavage of caspase-3 and poly (ADP-ribose) polymerase (PARP)-early markers of apoptosis[1].
Lirafugratinib (2h) 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 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) 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

509.53

Formula

C28H24FN7O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

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
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 : 62.5 mg/mL (122.66 mM; ultrasonic and warming and heat to 60°C; 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 1.9626 mL 9.8130 mL 19.6259 mL
5 mM 0.3925 mL 1.9626 mL 3.9252 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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Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.60%

COA (260 KB) HNMR (281 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
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 1.9626 mL 9.8130 mL 19.6259 mL 49.0648 mL
5 mM 0.3925 mL 1.9626 mL 3.9252 mL 9.8130 mL
10 mM 0.1963 mL 0.9813 mL 1.9626 mL 4.9065 mL
15 mM 0.1308 mL 0.6542 mL 1.3084 mL 3.2710 mL
20 mM 0.0981 mL 0.4906 mL 0.9813 mL 2.4532 mL
25 mM 0.0785 mL 0.3925 mL 0.7850 mL 1.9626 mL
30 mM 0.0654 mL 0.3271 mL 0.6542 mL 1.6355 mL
40 mM 0.0491 mL 0.2453 mL 0.4906 mL 1.2266 mL
50 mM 0.0393 mL 0.1963 mL 0.3925 mL 0.9813 mL
60 mM 0.0327 mL 0.1635 mL 0.3271 mL 0.8177 mL
80 mM 0.0245 mL 0.1227 mL 0.2453 mL 0.6133 mL
100 mM 0.0196 mL 0.0981 mL 0.1963 mL 0.4906 mL
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Lirafugratinib 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:

Lirafugratinib2549174-42-5RLY-4008RLY4008RLY 4008FGFRFibroblast growth factor receptororallyirreversiblecovalentlyCys491PARPInhibitorinhibitorinhibit

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