Canertinib

Title: Canertinib
CAS Registry Number: 267243-28-7
CAS Name: N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-2-propenamide
Additional Names: N-[4-(3-chloro-4-fluorophenylamino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]acrylamide
Molecular Formula: C24H25ClFN5O3
Molecular Weight: 485.94
Percent Composition: C 59.32%, H 5.19%, Cl 7.30%, F 3.91%, N 14.41%, O 9.88%
Literature References: Irreversible pan-erbB tyrosine kinase inhibitor. Prepn: A. J. Bridges et al., WO 0031048; eidem, US 6344455 (2000, 2002 both to Warner-Lambert); J. B. Smaill et al., J. Med. Chem. 43, 1380 (2000). Clinical pharmacokinetics in patients with solid malignancies: E. Calvo et al., Clin. Cancer Res. 10, 7112 (2004); and tolerability in refractory cancer: J. Nemunaitis et al., ibid. 11, 3846 (2005). Review of pharmacology and mechanism of action: L. F. Allen et al., Semin. Oncol. 30, Suppl. 16, 65-78 (2003); of development and clinical experience: C. M. Galmarini, IDrugs 7, 58-63 (2004).
Properties: Crystals from methanol, mp 188-190°.
Melting point: mp 188-190°
Derivative Type: Dihydrochloride
CAS Registry Number: 289499-45-2
Manufacturers' Codes: CI-1033
Molecular Formula: C24H25ClFN5O3.2HCl
Molecular Weight: 558.86
Percent Composition: C 51.58%, H 4.87%, Cl 19.03%, F 3.40%, N 12.53%, O 8.59%
Properties: Sol in water.
Therap-Cat: Antineoplastic.
Keywords: Antineoplastic; Tyrosine Kinase Inhibitors.
Canfosfamide Cangrelor Cannabinol Cantharidin Capobenic Acid

Canertinib
Canertinib.svg
Identifiers
CAS number 267243-28-7
PubChem 156414
ChemSpider 137741 YesY
UNII C78W1K5ASF YesY
ChEBI CHEBI:61399 YesY
ChEMBL CHEMBL31965
Jmol-3D images Image 1
Properties
Molecular formula C24H25ClFN5O3
Molar mass 485.94 g mol−1
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Except where noted otherwise, data are given for materials in their standard state (at 25 °C (77 °F), 100 kPa)
Infobox references

Canertinib (CI-1033) is an experimental drug candidate for the treatment of cancer. It is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM).[1][2]