1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. 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.

FGFR4-IN-20

FGFR4-IN-20 Chemical Structure

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Description

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[1].

IC50 & Target

FGFR4

 

Cellular Effect
Cell Line Type Value Description References
HS27 GI50
913 nM
Compound: 11
Growth inhibition of human HS27 cells by SRB assay
Growth inhibition of human HS27 cells by SRB assay
[PMID: 38706130]
Hep 3B2 GI50
16 nM
Compound: 11
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
[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
[PMID: 38706130]
HepG2 GI50
335 nM
Compound: 11
Growth inhibition of human HepG2 cells by SRB assay
Growth inhibition of human HepG2 cells by SRB assay
[PMID: 38706130]
Huh-7 GI50
16 nM
Compound: 11
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
Growth inhibition of human PLCPRF5 cells by SRB assay
Growth inhibition of human PLCPRF5 cells by SRB assay
[PMID: 38706130]
RT-112 GI50
151 nM
Compound: 11
Growth inhibition of FGFR3 overexpressing human RT-112 cells by SRB assay
Growth inhibition of FGFR3 overexpressing human RT-112 cells by SRB assay
[PMID: 38706130]
SNU-387 GI50
251 nM
Compound: 11
Growth inhibition of human SNU-387 cells by SRB assay
Growth inhibition of human SNU-387 cells by SRB assay
[PMID: 38706130]
In Vitro

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.

In Vivo

FGFR4-IN-20 (100mg/kg, p.o., QD for 15 d) significantly reduces the tumor volumes of ICR mice without a loss of body weight or other clinical signs[1].
1.19
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.

Molecular Weight

509.38

Formula

C26H22Cl2N4O3

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

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
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FGFR4-IN-20 Related Classifications

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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.

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Product Name:
FGFR4-IN-20
Cat. No.:
HY-163569
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