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Cat. No.: HY-143881

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FGFR4-IN-6

FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC₅₀ value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity. FGFR4-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

For research use only. We do not sell to patients.

CAS No.: 2760970-10-1
Formula: C₃₁H₃₃N₇O₄
Molecular Weight:567.64

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (266 KB)

FGFR4-IN-6 Chemical Structure

CAS No.: 2760970-10-1

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
Chemical Information
Purity & Documentation
References
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Bioz

Biological Activity

Description

FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC₅₀ value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity^[1]. FGFR4-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Cellular Effect

Cell Line	Type	Value	Description	References
Hep 3B2	IC₅₀	104.13 nM Compound: 9ka	Cytotoxicity against human Hep 3B2.1-7 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth Cytotoxicity against human Hep 3B2.1-7 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth	[PMID: 35119278]
Huh-7	IC₅₀	2.4 nM Compound: 9ka	Cytotoxicity against human Huh-7 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth Cytotoxicity against human Huh-7 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth	[PMID: 35119278]
MDA-MB-453	IC₅₀	140 nM Compound: 9ka	Cytotoxicity against human MDA-MB-453 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth Cytotoxicity against human MDA-MB-453 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth	[PMID: 35119278]
NCI-H1581	IC₅₀	>3 μM Compound: 9ka	Cytotoxicity against human NCI-H1581 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth Cytotoxicity against human NCI-H1581 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth	[PMID: 35119278]

Chemical Information

CAS No. 2760970-10-1
Molecular Weight 567.64
Formula C₃₁H₃₃N₇O₄
SMILES

O=C(N1CCCC2=CC(CN3C(CN(CC3)C)=O)=C(N=C21)C=O)NC4=CC(OC(C)C)=C(C=N4)C#CC5=CC=CN=C5
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (266 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Zhen Zhang, et al. Design, Synthesis, and Biological Evaluation of 2-Formyl Tetrahydronaphthyridine Urea Derivatives as New Selective Covalently Reversible FGFR4 Inhibitors. J Med Chem. 2022 Feb 24;65(4):3249-3265. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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