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
- 화학식: C31H33N7O4
- 분자량:567.64
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
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
-
분자량 567.64
-
화학식 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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선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)