Canertinib Dihydrochloride

Name: Canertinib Dihydrochloride
SKU: C0252
Availability: InStock

Product ID C0252

Cas No. 289499-45-2

Purity ≥98%

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Product Info
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Description

Canertinib is an irreversible inhibitor of EGFR (HER2/ErbB). This compound is currently in clinical trials as an anticancer chemotherapeutic, displaying activity against a variety of cancers. In a cellular model of melanoma, canertinib exhibits cytostatic activity, stopping cell growth in the G1 phase, but not inducing apoptosis except at very high concentrations. In a related animal model, canertinib inhibits tumor growth. Separately, canertinib inhibits Akt and ERK1/2 in cells lacking ErbB receptors and induces caspase-mediated apoptosis.

Product Info

Cas No.	289499-45-2
Purity	≥98%
Formula	C₂₄H₂₅ClFN₅O₃ • 2HCl
Formula Wt.	558.86
IUPAC Name	N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6- yl]prop-2-enamide;dihydrochloride
Synonym	CI1033
Appearance	Pale yellow powder

Shipping and Storage

Store Temp	Ambient
Ship Temp	Ambient

Downloads

MSDS	C0252 MSDS PDF
Info Sheet	C0252 Info Sheet PDF
Brochures	PI3K-Akt-mTORC Pathway Booklet
	Ras-Raf-MEK-ERK Pathway Booklet

References

Djerf Severinsson EA, Trinks C, Gréen H, et al. The pan-ErbB receptor tyrosine kinase inhibitor canertinib promotes apoptosis of malignant melanoma in vitro and displays anti-tumor activity in vivo. Biochem Biophys Res Commun. 2011 Oct 28;414(3):563-8. PMID: 21982771.

Trinks C, Severinsson EA, Holmlund B, et al. The pan-ErbB tyrosine kinase inhibitor canertinib induces caspase-mediated cell death in human T-cell leukemia (Jurkat) cells. Biochem Biophys Res Commun. 2011 Jul 8;410(3):422-7. PMID: 21669187.

Zinner RG, Nemunaitis J, Eiseman I, et al. Phase I clinical and pharmacodynamic evaluation of oral CI-1033 in patients with refractory cancer. Clin Cancer Res. 2007 May 15;13(10):3006-14. PMID: 17505003.