| Identification | Back Directory | [Name]
Canertinib dihydrochloride | [CAS]
289499-45-2 | [Synonyms]
CI103
CI 103
CI-1033
Canertinib HCl
Canertinib 2HC
Canertinib.2HCL
CI1033 dihydrochloride
CI-1033 dihydrochloride
CI 1033 dihydrochloride
PD-183805 dihydrochloride
Canertinib (CI-1033) HCl
Canertinib (CI-1033) 2HCl
Canertinib (hydrochloride)
CANERTINIB DIHYDROCHLORIDE
Canertinib dihydrochloride (CI-1033
Canertinib (CI-1033) dihydrochloride
Canertinib dihydrochloride USP/EP/BP
Canertinib dihydrochloride/Canertinib
Canertinib Dihydrochloride (CI-1033 HCl)
N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-morpholinopropoxy)quinazolin-6-yl)acrylamide dihydr
N-[4-(3-Chloro-4-fluorophenylamino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]acrylamide dihydrochloride
N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide dihydrochloride
N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-2-propenamide dihydrochloride
Canertinib dihydrochloride N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide dihydrochloride
CANERTINIB;CI-1033 DIHYDROCHLORIDE;PD-183805 DIHYDROCHLORIDE;CI1033 DIHYDROCHLORIDE;CI 1033 DIHYDROCHLORIDE;PD183805 DIHYDROCHLORIDE;PD 183805 DIHYDROCHLORIDE | [Molecular Formula]
C24H27Cl3FN5O3 | [MDL Number]
MFCD09954112 | [MOL File]
289499-45-2.mol | [Molecular Weight]
558.86 |
| Hazard Information | Back Directory | [Uses]
CI-1033 is a potent inhibitor of EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, respectively. | [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.
| [Biological Activity]
CI-1033 is a potentirreversible ATP binding site–directed pan-ErbB tyrosine kinase inhibitor with IC50 in the low nanomolar range for EGFRHER2and ErbB-4. | [in vivo]
Canertinib dihydrochloride (CI-1033 dihydrochloride) shows superior in vivo antitumor activity, giving growth delays in A431 xenografts exceeding 50 days following oral administration[1]. The growth of human malignant melanoma xenografts, RaH3 and RaH5, in nude mice is significantly inhibited by i.p. injections of 40 mg/kg/day canertinib (Fig. 4). The anti-proliferative effect on melanoma xenografts is visible already within 4 days of treatment and further increased throughout the treatment period as observed through the differences in tumor volumes, reaching statistical significance within 18 days of treatment[2]. | [IC 50]
EGFR: 7.4 nM (IC50); ErbB2: 9 nM (IC50) | [storage]
Store at -20°C |
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