FGFR-IN-19 

Arg-IN-1 is a selective Arginine (Arg)-targeting covalent inhibitor with IC₅₀s of 9.7 nM and 30.4 nM for FGFR2 and FGFR3,respectively. Arg-IN-1 has the potential to avoid FGFR1/4-targeted toxicity as well as conquer acquired on-target resistance, potential for FGFR-targeting cancer therapy^[1].

Arg-IN-1 (Compound RF3) has excellent selectivity for FGFR2 and FGFR3 with 244-fold and 765-fold lower inhibition of FGFR1 and FGFR4, respectively^[1].
Arg-IN-1 has superior anti-resistance activity with IC₅₀ of 9.4 nM against the FGFR2 V564F mutation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

738.80

C₃₆H₄₂N₁₂O₆

COCCNC1=NC(NC2=NNC(C3=CC=CC=C3)=C2)=NC(NC4CC5(C4)CCN(CC5)C(CN6C=C(N=N6)COC7=CC=C(C=C7)C(C(O)O)=O)=O)=N1

Room temperature in continental US; may vary elsewhere.

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

• [1]. Wu X, et al. Residue-Selective Inhibitors Discovery via Covalent DNA-Encoded Chemical Libraries with Diverse Warheads. J Am Chem Soc. 2025 May 7; 147(18):15469-15481.  [Content Brief]