Shelf life (days): 1460.0
Formulation: A solid
Formal Name: (2E)-N-[4-[[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
Purity: ≥98%
Formula Markup: C31H29ClFN5O3
Formula Weight: 574.1
CAS Number: 848133-17-5
Notes: HKI 357 is an irreversible dual inhibitor of the EGF receptor tyrosine kinases EGFR and HER2 (IC50s = 34 and 33 nM, respectively).{39458} It inhibits proliferation of A431, SK-BR-3, and SW620 cancer cell lines (IC50s = 120, 2.5, and 511 nM, respectively). HKI 357 suppresses EGFR autophosphorylation and phosphorylation of the downstream effectors AKT and ERK in the gefitinib-susceptible and -resistant cell lines NCI-H1650 and NCI-H1650(G7), respectively.{30795} In vivo, HKI 357 (10 mg/kg) inhibits tumor growth in BT474, A431, and SUM190 mouse xenograft models.{39458}