 Home > Encyclopedia > Canertinib

Canertinib

Canertinib structure

CAS No:
267243-28-7
Formula:
C24H25ClFN5O3
Chemical Name:
Canertinib
Synonyms:
2-Propenamide,N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-;N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-2-propenamide;Canertinib;N-[4-(3-Chloro-4-fluorophenylamino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]acrylamide;Cl 1033;4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-(morpholin-4-yl)propyloxy]-6-[(vinylcarbonyl)amino]quinazoline
Categories:
Active Pharmaceutical Ingredients > Antineoplastic Agents

Description

Canertinib (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 is a quinazoline compound having a 3-chloro-4-fluoroanilino group at the 4-position, a propenamido group at the 6-position, and a 3-morpholinopropoxy group at the 7-position. It has a role as a tyrosine kinase inhibitor and an antineoplastic agent. It is a member of quinazolines, an organofluorine compound, a member of morpholines and a member of monochlorobenzenes.|Canertinib is a pan-erbB tyrosine kinase inhibitor which work against esophageal squamous cell carcinoma in vitro and in vivo. Canertinib treatment significantly affects tumour metabolism, proliferation and hypoxia as determined by PET.

Canertinib Basic Attributes

Molecular Weight：

485.944

Exact Mass：

485.94

EC Number：

1308068-626-2

UNII：

C78W1K5ASF

DSSTox ID：

DTXSID8048943

Characteristics

PSA：

88.6

XLogP3：

3.9

Appearance：

white or similar to white crystalline powder

Density：

1.4±0.1 g/cm3

Melting Point：

188-190°

Boiling Point：

691.0±55.0°C at 760 mmHg

Flash Point：

371.7±31.5 °C

Refractive Index：

1.650

Vapor Pressure：

2.86E-18mmHg at 25°C

Drug Information

Drug Indication：

Investigated for use/treatment in breast cancer and lung cancer.

Mechanism of Action：

CI-1033 effectively inhibits the growth of esophageal squamous cell carcinoma which co-expresses both EGFR and HER2 with the inhibition of phosphorylation of both MAPK and AKT. Some studies suggest that CI-1033 holds significant clinical potential in esophageal cancer.

MeSH Entry Terms：

Canertinib

Canertinib Use and Manufacturing

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

Computed Properties

Molecular Weight:485.9
XLogP3:3.9
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:8
Rotatable Bond Count:9
Exact Mass:485.1629955
Monoisotopic Mass:485.1629955
Topological Polar Surface Area:88.6
Heavy Atom Count:34
Complexity:671
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Recommended Suppliers of Canertinib

LEAP CHEM CO., LTD. Contact Supplier

CN
4 YRS

Business licensed

Trader Supplier of Intermediates,Building blocks,API,Silicones,Peptides,Lab chemicals,Biochemicals,Pharmaceuticals,Screening Compounds,Food Additives

Canertinib

CAS No.: 267243-28-7

Content: 99.00%

Inquiry
Creative Enzymes Contact Supplier

US
5 YRS

Business licensed Certified factory

Manufactory Supplier of Coenzymes,Inhibito,Enzymes,Zymogens,Substrates

CI-1033(Canertinib)

CAS No.: 267243-28-7

Content: 99%

Inquiry
Jinan Wonder Pharmtech Co., Ltd Contact Supplier

CN
3 YRS

Business licensed

Trader Supplier of Pharmaceutical Intermediates

Canertinib 99%

CAS No.: 267243-28-7

Content: 99%

Inquiry
Chongqing Chemdad Contact Supplier

CN
2 YRS

Business licensed

Trader Supplier of Amino acid,intermediates

Canertinib

CAS No.: 267243-28-7

Inquiry

54 Suppliers of Canertinib