Canertinib dihydrochloride
-
Canertinib dihydrochloride
structure -
-
CAS No:
289499-45-2
-
Formula:
C24H25ClFN5O3.2ClH
-
Chemical Name:
Canertinib dihydrochloride
-
Synonyms:
2-Propenamide,N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-,hydrochloride (1:2);2-Propenamide,N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-,dihydrochloride;PD 183805;Canertinib dihydrochloride;CI 1033;338796-35-3
- Categories:
-
CAS No:
Description
Canertinib dihydrochloride (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.
Canertinib Dihydrochloride is the hydrochloride salt of an orally bio-available quinazoline with potential antineoplastic and radiosensitizing activities. Canertinib binds to the intracellular domains of epidermal growth factor receptor tyrosine kinases (ErbB family), irreversibly inhibiting their signal transduction functions and resulting in tumor cell apoptosis and suppression of tumor cell proliferation. This agent also acts as a radiosensitizing agent and displays synergistic activity with other chemotherapeutic agents.
Safety Information
NONH for all modes of transport
3
36/37/38
26
UC6316110
Xi
P261-P305 + P351 + P338
H315-H319-H335
|Warning|H315 (100%): Causes skin irritation [Warning Skin corrosion/irritation]|P261, P264, P271, P280, P302+P352, P304+P340, P305+P351+P338, P312, P321, P332+P313, P337+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 38 companies from 1 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
Drug Information
Substances that inhibit or prevent the proliferation of NEOPLASMS. (See all compounds classified as Antineoplastic Agents.)|Agents that have a strengthening effect on the heart or that can increase cardiac output. They may be CARDIAC GLYCOSIDES; SYMPATHOMIMETICS; or other drugs. They are used after MYOCARDIAL INFARCT; CARDIAC SURGICAL PROCEDURES; in SHOCK; or in congestive heart failure (HEART FAILURE). (See all compounds classified as Cardiotonic Agents.)|Drugs that block nerve conduction when applied locally to nerve tissue in appropriate concentrations. They act on any part of the nervous system and on every type of nerve fiber. In contact with a nerve trunk, these anesthetics can cause both sensory and motor paralysis in the innervated area. Their action is completely reversible. (From Gilman AG, et. al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed) Nearly all local anesthetics act by reducing the tendency of voltage-dependent sodium channels to activate. (See all compounds classified as Anesthetics, Local.)
canertinib dihydrochloride
Canertinib dihydrochloride Use and Manufacturing
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 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 also displays anti-neoplastic activity towards T98G glioblastoma cells, HCT8 colorectal carcinoma cells, and cells expressing the breast cancer resistance protein.
Computed Properties
Molecular Weight:558.9
Hydrogen Bond Donor Count:4
Hydrogen Bond Acceptor Count:8
Rotatable Bond Count:9
Exact Mass:557.116351
Monoisotopic Mass:557.116351
Topological Polar Surface Area:88.6
Heavy Atom Count:36
Complexity:671
Covalently-Bonded Unit Count:3
Compound Is Canonicalized:Yes
Recommended Suppliers of Canertinib dihydrochloride
-
![China]()
CN
5 YRS
Business licensedTrader Supplier of Intermediates,Building blocks,API,Silicones,Peptides,Lab chemicals,Biochemicals,Pharmaceuticals,Screening Compounds,Food Additives -
![United States]()
US
6 YRS
Business licensed Certified factoryManufactory Supplier of Coenzymes,Inhibito,Enzymes,Zymogens,Substrates -
![China]()
CN
4 YRS
Business licensedTrader Supplier of Pharmaceutical Intermediates
Learn More Other Chemicals
-
Benzenecarboximidamide, 4,4′-iminobis-, dihydrochloride
21055-30-1
-
2,3-diaMino-5-broMobenzoic acid dihydrochloride
58580-09-9
-
Glycine, N-2-naphthalenyl-, hydrazide, dihydrochloride
70700-31-1
-
L-Cystine, radical ion(1+), dihydrochloride Formula
13059-63-7
-
1-(3,4-DICHLORO-BENZYL)-PYRROLIDIN-3-YLAMINE DIHYDROCHLORIDE Formula
828928-33-2
-
Dibromopropamidine Dihydrochloride Formula
50357-61-4
-
1-(2,4-DICHLOROPHENYL)-PIPERAZINE DIHYDROCHLORIDE Structure
827614-48-2
-
2-CYCLOHEXYL-1 H-BENZOIMIDAZOL-5-YLAMINE DIHYDROCHLORIDE Structure
1158326-68-1
-
What is D-Leucine, N2-(3,7-dimethyl-1-oxooctyl)-L-lysyl-L-lysyl-L-threonyl-L-lysyl-, cyclic (5->2)-peptide, dihydrochloride 5CAS:85830-18-8Purity:98% HPLC Package:5mg;1G;10G;100G;1KG
85830-18-8
-
What is Streptomycin, dihydro-, dihydrochloride
884483-17-4