Ellence Inhibitor CAS No. 56390-09-1

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Chemical Characteristic

Product Name	Ellence
Synonyms	Epirubicin Hydrochloride, Pharmorubicin, Epirubicin Ebewe
CAS No.	56390-09-1
Molecular Weight	579.98
Formula	C₂₇H₂₉NO₁₁HCl
Chemical Name	(7S,9S)-7-[(2R,4S,5R,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy-6,9,11-trihydroxy-9-(2-hydroxyacetyl)-4-methoxy-8,10-dihydro-7H-tetracene-5,12-dione;hydrochloride
Smiles	c1ccc2c(c1OC)C(=O)c1c(C2=O)c(c2c(c1O)[C@H](C[C@@](C2)(C(=O)CO)O)O[C@H]1C[C@@H]([C@H]([C@@H](O1)C)O)N)O Cl
Chemical Structure

Biological activities

Ellence is an anthracycline cytostatic antibiotic with the wide antineoplastic spectrum and high efficiency. Ellence is also one of the most active cytostatics applied in breast cancer therapy, which acts as an agent intercalating between bases of double-stranded DNA thereby interrupting DNA transcription and replication. Ellence exhibits significant dose- and time-dependent inhibition of the growth of MDA-MB-231 cells, with an IC50 of 8 µM. ^[1] In addition, ellence is exported by MDR1 protein of hepatic cancer cells. Ellence inhibits HepG2 cells with IC50 of 23.5 µM in spheroid culture, and 7.8 µM in monolayer culture. ^[2] Ellence cyctotoxic effects involve the formation of intracellular free radicals caused by the quinone group of antracycline. Ellence inhibits MCF-7WT and EPIR tumor cells with IC50 of 1.2 ng/mL and 0.5 µg/mL, respectively. Ellence can induce the expression of P-gp in MCF-7 cells.^[3] In xenografted MDA-MB-231 cells in nude mice, ellence (4 mg/kg) remarkably inhibits tumor growth.^[1]

Protocols

Ellence is dissolved in isotonic saline solution immediately before use in vitro assays.^[1]

References

[1] Yamamoto D, et al. Synergistic effects induced by cycloprodigiosin hydrochloride and epirubicin on human breast cancer cells. Breast Cancer Res Treat. 2002, 72 (1): 1-10. [2] Oshikata A, et al. Enhancement of drug efflux activity via MDR1 protein by spheroid culture of human hepatic cancer cells. J Biosci Bioeng. 2011, 111(5): 590-593. [3] Ozkan A, et al. Combined effect of epirubicin and lymphokine-activated killer cells on the resistant human breast cancer cells. Cell Biol Toxicol. 2004, 20(5): 261-271.

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