HKI-357 dimaleate 

HKI-357 dimaleate is an irreversible dual inhibitor of EGFR and ERBB2 with IC₅₀s of 34 nM and 33 nM, respectively. HKI-357 dimaleate suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation^[1].

HKI-357 (0.01-10 μM) is effective in suppressing ligand-induced EGFR autophosphorylation and its downstream signaling, as determined by AKT and MAPK phosphorylation in NCI-H1975 cells^[1].
HKI-357 also is effective in suppressing EGFR autophosphorylation (measured at residue Y1068), and AKT and MAPK phosphorylation in parental NCI-H1650 cells harboring the delE746-A750 EGFR mutation^[1].

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

806.19

C₃₉H₃₇ClFN₅O₁₁

915942-25-5

OC(/C=C\C(O)=O)=O.CCOC(C(NC(/C=C/CN(C)C)=O)=C1)=CC2=C1C(NC3=CC(Cl)=C(C=C3)OCC4=CC(F)=CC=C4)=C(C#N)C=N2.OC(/C=C\C(O)=O)=O

Room temperature in continental US; may vary elsewhere.

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

• [1]. Kwak EL, et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci U S A. 2005 May 24;102(21):7665-70.  [Content Brief]