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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.

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CAS No.: 2760970-10-1
Formule: C₃₁H₃₃N₇O₄
Masse moléculaire:567.64

Stockage:

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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Use of MCE Products

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

Activité biologique
- Description
- Cellular Effect
Chemical Information
Pureté et documentation
Références
Calculators
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Activité biologique

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
Masse moléculaire 567.64
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
Instruction de manipulation (2659 KB)

Références

[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]

Calculators

Calculateur de molarité

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Molecular Weight Molecular Weight

Calculateur de dilution

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Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

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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.

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MOQ

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100 mg

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