FGFR4-IN-19
FGFR4-IN-19 (compound 8B) is a potent covalent fibroblast growth factor receptor 4 (FGFR4) inhibitor (IC50=1.2 nM). FGFR4-IN-19 achieves high efficiency and isotype selectivity by covalently targeting a rare cysteine (C552) in the FGFR4 kinase domain. FGFR4-IN-19 can be used for hepatocellular carcinoma (HCC) research.
For research use only. We do not sell to patients.
- CAS No.: 3036751-84-2
- Formula: C21H14Cl3N5O4
- Molecular Weight:506.73
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
FGFR4 1.2 nM (IC50) |
FGFR1 4370 nM (IC50) |
FGFR2 490 nM (IC50) |
FGFR3 >5000 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Hep 3B2 | EC50 |
22 nM
Compound: 8B
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Antiproliferative activity against human Hep3B cells measured after 4 days by Celltiter-glo based luminescent assay
Antiproliferative activity against human Hep3B cells measured after 4 days by Celltiter-glo based luminescent assay
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[PMID: 38604131] |
In Vitro
FGFR4-IN-19 shows weak inhibitory activity for FGFR1 (IC50=4.4 μM) and FGFR2 (IC50=490 nM), while all other IC50 values were above 5 μM. FGFR4-IN-19 has highly selective within the FGFR family[1].
FGFR4-IN-19 shows potent cellular FGFR4 engagement (EC50=52±7 nM) compared to the FGFR1-3 (EC50＞10 μM)[1].
FGFR4-IN-19 (0.3 μM, 24 h) shows good antiproliferative activity and blocks efficiently the FRS2 phosphorylation in Hep3B cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 3036751-84-2
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Molecular Weight 506.73
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Formula C21H14Cl3N5O4
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SMILES
ClC(N=C1NC2=NC=C3C(C=CC(C4=C(C(OC)=CC(OC)=C4Cl)Cl)=C3)=N2)=CC=C1[N+]([O-])=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Liver Cancer Modeling
Liver cancer can be classified into primary liver cancer and secondary liver cancer. Secondary liver cancer is the metastatic liver cancer. Primary liver cancer includes hepatocellular carcinoma (HCC), intrahepatic cholangiocarcinoma (ICC) and fibrolamellar HCC, of which HCC is the most common form, accounting for approximately 90% of primary liver cancers[1]. HCC mouse models include chemical agent-induced models, transplanted tumor models, and genetic engineered models.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FGFR4-IN-19 Related Classifications
HY-158248 Related Classifications
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