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
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
FGFR4 1.2 nM (IC50) |
FGFR1 4370 nM (IC50) |
FGFR2 490 nM (IC50) |
FGFR3 >5000 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Hep 3B2 | EC50 |
22 nM
Compound: 8B
|
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
|
[PMID: 38604131] |
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.
Chemical Information
-
CAS No. 3036751-84-2
-
Molecular Weight 506.73
-
Formula C21H14Cl3N5O4
-
SMILES
ClC(N=C1NC2=NC=C3C(C=CC(C4=C(C(OC)=CC(OC)=C4Cl)Cl)=C3)=N2)=CC=C1[N+]([O-])=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FGFR4-IN-19 Related Classifications
HY-158248 Related Classifications
Powered by Bioz