FGFR4-IN-8

Cat. No.: HY-145836: FAQs
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FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4^V550L, FGFR4^V550M and FGFR4^C552S with IC₅₀s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC₅₀ value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model.

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

FGFR4-IN-8 Chemical Structure

CAS No. : 2765240-52-4

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Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	> 1 μM Compound: 7v	Antiproliferative activity against mouse BAF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35271262]
BaF3	IC₅₀	0.0035 μM Compound: 7v	Antiproliferative activity against mouse BAF3 cells expressing wild-type FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells expressing wild-type FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35271262]
BaF3	IC₅₀	4.7 nM Compound: 7v	Antiproliferative activity against mouse BAF3 cells expressing FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells expressing FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35271262]
BaF3	IC₅₀	8.1 nM Compound: 7v	Antiproliferative activity against mouse BAF3 cells expressing FGFR4 V550M mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells expressing FGFR4 V550M mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35271262]
Hep 3B2	IC₅₀	0.029 μM Compound: 7v	Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 5 days by SRB assay Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 5 days by SRB assay	[PMID: 35271262]
Huh-7	IC₅₀	72 nM Compound: 7v	Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay	[PMID: 35271262]
MDA-MB-453	IC₅₀	0.034 μM Compound: 7v	Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay	[PMID: 35271262]
NCI-H1299	IC₅₀	2.97 μM Compound: 7v	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay	[PMID: 35271262]

Molecular Weight

654.56

Formula

C₃₂H₃₄Cl₂FN₇O₃

CAS No.

2765240-52-4

SMILES

C[C@@H](OC1=CC=C(C2=C1)NN=C2NC3=C(C=C(C=C3F)N4CCC(CC4)N5CCOCC5)NC(C=C)=O)C6=C(C=NC=C6Cl)Cl

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

Handling Instructions (2659 KB)

References

[1]. Min Shao, et al. Design, Synthesis, and Biological Evaluation of Aminoindazole Derivatives as Highly Selective Covalent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR4. J Med Chem. 2022 Mar 24;65(6):5113-5133. [Content Brief]

FGFR4-IN-8 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.

Keywords:

FGFR4-IN-82765240-52-4FGFRFibroblast growth factor receptorATP-competitivecovalentwild-typegatekeeper mutantFGFR4Hep3B hepatocellular carcinoma cellsHuh-7 xenograftInhibitorinhibitorinhibit

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