Canertinib dihydrochloride Chemical Properties

storage temp. 

Sealed in dry,Store in freezer, under -20°C

solubility 

DMSO: >10mg/mL

form 

solid

Safety Information

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

26

WGK Germany 

3

RTECS 

UC6316110

Canertinib dihydrochloride Usage And Synthesis

Uses

CI-1033 is a potent inhibitor of EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, respectively.

Uses

Canertinib Dihydrochloride is a water-soluble, EGFR, HER2, and ErbB-4 tyrosine kinase inhibitor.

Uses

The HER family of receptor tyrosine kinases, EGFR, HER2, HER3, and HER4, mediate proliferation, migration, adhesion, differentiation, and survival in many different cell types and have been implicated in the development and progression of a variety of human tumors.Canertinib dihydrochloride is an irreversible quinazoline-based HER family tyrosine kinase inhibitor with IC50 values of 0.8, 19, and 7 nM for blocking in vitro activity of EGFR, HER2, and HER4, respectively. As a broadly applicable anti-cancer agent, it has been used to suppress proliferation of malignant peripheral nerve sheath tumor cells (effective concentration of 250-500 nM), to inhibit growth and induce dose-dependent apoptosis in a panel of neuroblastoma cell lines (IC50s = 0.94-2.45 μM), and to reduce proliferation of acute myeloid leukemia cells (IC50 = 0.27 μM). Canertinib dihydrochloride also displays anti-neoplastic activity towards T98G glioblastoma cells, HCT8 colorectal carcinoma cells, and cells expressing the breast cancer resistance protein.

storage

Store at -20°C

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