Products Details

Product Description

– 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].

Web ID

– HY-145836

Shipping

– Room temperature

Applications

– Cancer-Kinase/protease

Molecular Formula

– C32H34Cl2FN7O3

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.

CAS Number

– 2765240-52-4

Molecular Weight

– 654.56

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

Clinical Information

– No Development Reported

Research Area

– Cancer

Solubility

– 10 mM in DMSO

Target

– FGFR

Pathway

– Protein Tyrosine Kinase/RTK

Product type

– Reference compound

Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.

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