Canertinib dihydrochloride |CAS:289499-45-2 Probechem Biochemicals

Chemical Structure : Canertinib dihydrochloride

CAS No.: 289499-45-2

Canertinib dihydrochloride (Canertinib;CI-1033 dihydrochloride;PD-183805 dihydrochloride;CI1033 dihydrochloride;CI 1033 dihydrochloride;PD183805 dihydrochloride;PD 183805 dihydrochloride)

Catalog No.: PC-42553Not For Human Use, Lab Use Only.

Canertinib dihydrochloride (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.

Packing	Price	Stock
25 mg	$148	In stock
50 mg	$198	In stock
100 mg	$288	In stock
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Biological Activity

Canertinib dihydrochloride (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 dihydrochloride (CI-1033, PD183805) displays no activity to PDGFR, FGFR, InsR, PKC, and CDK1/2/4.
Canertinib dihydrochloride (CI-1033, PD183805) 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 dihydrochloride (CI-1033, PD183805) shows high in vivo activity against A431 xenografts.

Physicochemical Properties

M.Wt	558.8603
Formula	C24H27Cl3FN5O3
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	2-Propenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-, hydrochloride (1:2)

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.

4. Slichenmyer WJ, et al. Semin Oncol. 2001 Oct;28(5 Suppl 16):80-5.

Canertinib dihydrochloride (Canertinib;CI-1033 dihydrochloride;PD-183805 dihydrochloride;CI1033 dihydrochloride;CI 1033 dihydrochloride;PD183805 dihydrochloride;PD 183805 dihydrochloride)

Biological Activity

Physicochemical Properties

References

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