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. |