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Canertinib

Chemical Structure : Canertinib

CAS No.: 267243-28-7

Canertinib (CI-1033, PD-183805)

Catalog No.: PC-23843Not For Human Use, Lab Use Only.

Canertinib (CI-1033, PD183805) is a potent, irreversible, orally available pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 7.5 nM and 9.0 nM in autophosphorylation assay.

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Biological Activity

Canertinib (CI-1033, PD183805) is a potent, irreversible, orally available pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 7.5 nM and 9.0 nM in autophosphorylation assay.
Canertinib displays no activity to PDGFR, FGFR, InsR, PKC, and CDK1/2/4.
Canertinib suppresses heregulin-stimulated tyrosine phosphorylation of erbB2, erbB3 and erbB4 with IC50 of 5, 14 and 10 nM, respectively, also inhibits expression of pp62c-fos in response to heregulin.
Canertinib shows high in vivo activity against A431 xenografts.

Physicochemical Properties

M.Wt 485.94
Formula C24H25ClFN5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-morpholinopropoxy)quinazolin-6-yl)acrylamide

References

1. Smaill JB, et al. J Med Chem. 2000 Apr 6;43(7):1380-97.

2. Erlichman C, et al. Cancer Res. 2001 Jan 15;61(2):739-48.

3. Nyati MK, et al. Clin Cancer Res. 2004 Jan 15;10(2):691-700.

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