| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 500mg | |||
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| Targets |
Lirafugratinib targets fibroblast growth factor receptor 2 (FGFR2), a receptor tyrosine kinase involved in cell proliferation and survival. The compound binds irreversibly to the ATP-binding site of FGFR2, specifically covalently modifying Cys491. This prevents FGFR2 activation and subsequent signaling. The compound is highly selective for FGFR2, with minimal activity against other FGFR family members.
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| ln Vitro |
In vitro, Lirafugratinib is a highly potent and selective FGFR2 inhibitor with an IC50 of 3 nM. It covalently binds to Cys491. The compound targets FGFR2 alterations and resistance mutations. Specific cellular assay data, such as effects on cell proliferation in FGFR2-dependent cell lines, are not detailed in the available sources.
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| ln Vivo |
In vivo, Lirafugratinib induces tumor regression in preclinical models. As an orally active compound, it is suitable for oral administration in cancer therapy. Specific in vivo study details, such as dosing regimens and tumor models, are not provided in the available sources.
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| Enzyme Assay |
A cell-free assay for Lirafugratinib would involve measuring its inhibition of FGFR2 kinase activity. Recombinant FGFR2 is incubated with a peptide substrate and ATP in the presence of varying concentrations of the compound. The incorporation of phosphate into the substrate is measured, and IC50 values are calculated. For Lirafugratinib, the IC50 for FGFR2 is 3 nM.
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| Cell Assay |
Cellular assays for Lirafugratinib would typically involve assessing its effects on FGFR2-dependent cell proliferation and signaling. Cells with FGFR2 alterations are treated with the compound, and cell viability is measured. The inhibition of FGFR2 phosphorylation and downstream signaling can be assessed by Western blotting.
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| Animal Protocol |
In vivo animal experiments with Lirafugratinib have been conducted in preclinical tumor models. The compound induces tumor regression. Specific dosing regimens, animal models, and outcome measures are not provided in the available sources.
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| ADME/Pharmacokinetics |
Lirafugratinib is an orally active compound. It has a molecular formula of C28H24FN7O2 and a molecular weight of 509.53. Specific pharmacokinetic parameters, such as half-life and bioavailability, are not provided in the available sources. The compound is being developed for cancer therapy.
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| Toxicity/Toxicokinetics |
Toxicity data for Lirafugratinib are not provided in the available sources. As a research compound, it is intended for research use only and not for human consumption. Standard laboratory safety precautions should be observed when handling this compound.
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| References | |
| Additional Infomation |
Lirafugratinib is an orally bioavailable fibroblast growth factor receptor 2 (FGFR2) inhibitor with potential antitumor activity. After oral administration, Lirafugratinib binds to FGFR2 and inhibits its activity, thereby suppressing the FGFR2-mediated signal transduction pathway. This can inhibit the proliferation of FGFR2-overexpressing tumor cells. FGFR2 is a receptor tyrosine kinase that is upregulated in various tumor cell types and plays a crucial role in cell proliferation, migration, and survival.
Lirafugratinib (CAS: 2549174-42-5) is an orally active, irreversible, and highly selective FGFR2 inhibitor with an IC50 of 3 nM. It is also known as RLY-4008 and FGFR2-IN-3. The compound covalently binds to Cys491 and targets FGFR2 alterations and resistance mutations. Its molecular formula is C28H24FN7O2 and its molecular weight is 509.53. It is not an approved drug and is strictly for research purposes. |
| Molecular Formula |
C28H24FN7O2
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|---|---|
| Molecular Weight |
509.534268379211
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| Exact Mass |
509.197
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| CAS # |
2549174-42-5
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| Related CAS # |
Lirafugratinib hydrochloride;2688040-45-9
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| PubChem CID |
155309155
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
38
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| Complexity |
840
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1=C(C=CC(=C1)C1C2=C(N)N=CN=C2N(C)C=1C1C=CC(=CC=1)NC(C(=C)C)=O)OC1N=CC=C(C)N=1
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| InChi Key |
XOQVZSSDIQQUGO-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
N-[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
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~122.66 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1963 mL | 0.9813 mL | 1.9626 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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