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Chemical Structure : Canertinib dihydrochloride
CAS No.: 289499-45-2
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 | Quantity |
|---|---|---|---|
| 25 mg | $148 | In stock | |
| 50 mg | $198 | In stock | |
| 100 mg | $288 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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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.
| M.Wt | 558.8603 | |
| Formula | C24H27Cl3FN5O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-Propenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-, hydrochloride (1:2) |
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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.
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