An irreversible dual inhibitor of EGFR and HER2 (IC50s = 34 and 33 nM

HKI 357 – 10 mg

Brand:
Cayman
CAS:
848133-17-5
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

An irreversible dual inhibitor of EGFR and HER2 (IC50s = 34 and 33 nM, respectively); inhibits proliferation of A431, SK-BR-3, and SW620 cancer cell lines (IC50s = 120, 2.5, and 511 nM, respectively); suppresses EGFR autophosphorylation and phosphorylation of the downstream effectors AKT and ERK in NCI-H1650 and NCI-H1650(G7) cells; inhibits tumor growth in BT474, A431, and SUM190 mouse xenograft models (10 mg/kg) ,

Formal name: (2E)-N-[4-[[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide

Synonyms: 

Molecular weight: 574.1

CAS: 848133-17-5

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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