PeptideDB

HKI-357 dimaleate

CAS: 915942-25-5 F: C39H37ClFN5O11 W: 806.19

HKI-357 dimaleate is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-3
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Bioactivity 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].
Invitro 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> HKI-357 dimaleate 相关抗体: Western Blot Analysis[1] Cell Line:
CAS 915942-25-5
Formula C39H37ClFN5O11
Molar Mass 806.19
Transport Room temperature in continental US; may vary elsewhere.
Storage

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

Reference [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.