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FGFR4-IN-8

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, FGFR4V550L, FGFR4V550M and FGFR4C552S 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[1].

Product Specifications

CAS Number

2765240-52-4

UNSPSC

12352005

Target

FGFR

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/fgfr4-in-8.html

Solubility

10 mM in DMSO

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

Molecular Formula

C32H34Cl2FN7O3

Molecular Weight

654.56

References & Citations

[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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Frequently Asked Questions

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