FGFR4-IN-20
FGFR4-IN-20 (comp 11) is an orally active and selective FGFR4 inhibitor with IC50s of 19 and 36 nM against Huh7 cells and FGFR4 enzyme. FGFR4-IN-20 can be used for hepatocellular carcinoma research.
For research use only. We do not sell to patients.
- Formula: C26H22Cl2N4O3
- Molecular Weight:509.38
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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FGFR4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hep 3B2 | GI50 |
16 nM
Compound: 11
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Growth inhibition of FGF19 amplified and FGFR4 overexpressing human Hep3B cells by SRB assay
Growth inhibition of FGF19 amplified and FGFR4 overexpressing human Hep3B cells by SRB assay
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[PMID: 38706130] |
| Hep 3B2 | IC50 |
16 nM
Compound: 11
|
Antiproliferative activity against FGF19 amplified human Hep3B cells assessed as inhibition of cell growth by SRB assay
Antiproliferative activity against FGF19 amplified human Hep3B cells assessed as inhibition of cell growth by SRB assay
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[PMID: 38706130] |
| HepG2 | GI50 |
335 nM
Compound: 11
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Growth inhibition of human HepG2 cells by SRB assay
Growth inhibition of human HepG2 cells by SRB assay
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[PMID: 38706130] |
| HS27 | GI50 |
913 nM
Compound: 11
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Growth inhibition of human HS27 cells by SRB assay
Growth inhibition of human HS27 cells by SRB assay
|
[PMID: 38706130] |
| Huh-7 | GI50 |
16 nM
Compound: 11
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Growth inhibition of FGF19 amplified and FGFR4 overexpressing human Huh-7 cells by SRB assay
Growth inhibition of FGF19 amplified and FGFR4 overexpressing human Huh-7 cells by SRB assay
|
[PMID: 38706130] |
| Huh-7 | IC50 |
19 nM
Compound: 11
|
Antiproliferative activity against FGFR4 overexpressing human Huh-7 cells assessed as inhibition of cell growth by SRB assay
Antiproliferative activity against FGFR4 overexpressing human Huh-7 cells assessed as inhibition of cell growth by SRB assay
|
[PMID: 38706130] |
| PLC-PRF-5 | GI50 |
598 nM
Compound: 11
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Growth inhibition of human PLCPRF5 cells by SRB assay
Growth inhibition of human PLCPRF5 cells by SRB assay
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[PMID: 38706130] |
| RT-112 | GI50 |
151 nM
Compound: 11
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Growth inhibition of FGFR3 overexpressing human RT-112 cells by SRB assay
Growth inhibition of FGFR3 overexpressing human RT-112 cells by SRB assay
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[PMID: 38706130] |
| SNU-387 | GI50 |
251 nM
Compound: 11
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Growth inhibition of human SNU-387 cells by SRB assay
Growth inhibition of human SNU-387 cells by SRB assay
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[PMID: 38706130] |
FGFR4-IN-20 (0.01-1000 nM) shows IC50s of 19, 16 and 33 nM against Huh7 (FGFR4 overexpression), Hep3B (FGF19 amplification) and JHH-7 (FGF19 amplification) cell lines, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetics Profile of FGFR4-IN-20 in ICR Mice[1]
| Parameter | IV (5 mg/kg) | PO (100 mg/kg, QD) |
| AUC0-24 (ng·h/mL) | 4810 | 59534 |
| Cmax (ng/mL) | 8137 | 24566 |
| Tmax (h) | 0.5 | |
| T1/2 (h) | 1.7 | 3.9 |
| F% | 61.9 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 509.38
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Formula C26H22Cl2N4O3
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SMILES
ClC1=C(C2=CC3=CN=C(C=C3C(C)=N2)NC4=C(C=CC=C4)NC(C=C)=O)C(Cl)=C(OC)C=C1OC
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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