| Identification | Back Directory | [Name]
SM 5887 | [CAS]
110311-30-3 | [Synonyms]
Calsed
SM 5887
AMR hydrochloride
Amrubicin hydrochloride
BHMLHEQFWVQAJS-IERVSNJOSA-N
(1S,3S)-3-Acetyl-3-amino-5,12-dihydroxy-6,11-dioxo-1,2,3,4,6,11-hexahydro-1-tetracenyl2-deoxy-β-D-erythro-pentopyranosidehydrochloride(1:1)
(7S,9S)-9-Acetyl-9-amino-7-(2-deoxy-β-D-erythro-pentopyranosyloxy)-6,11-dihydroxy-5,7,8,9,10,12-hexahydro-5,12-naphthacenedione·hydrochloride | [Molecular Formula]
C25H25NO9.ClH | [MOL File]
110311-30-3.mol | [Molecular Weight]
519.931 |
| Hazard Information | Back Directory | [Description]
small and small-cell lung cancers. Amrubicin, a completely synthetic anthracycline
derivative, mediates its growth inhibitory action via topoisomerase II inhibition. It is
activated in viva by the formation of its 13-OH metabolite, amrubicinol, via reaction with
carbonyl reductase. In contrast to doxorubicin and daunorubicin whose metabolites are
inactive in the blood, amrubicinol is 10-100 fold more cytotoxic than amrubicin. In phase II
clinical trials, amrubicin showed antitumor activity against non-small-cell lung cancers
(response rate exceeding 20%) and against untreated extensive stage small-cell-lung
cancers (response rate 78.8%). Amrubicin demonstrated a smaller distribution-volume, a
shorter half-life in mice and also less chronic cardiotoxicity in preclinical studies compared
to doxorubicin. Amrubicin was generally well tolerated with major adverse events being
anaemia, leucopenia, thrombocytopenia and neutropenia. | [Originator]
Sumitomo (Japan) | [Uses]
Amrubicin (SM-5887) hydrochloride is a DNA topoisomerase II inhibitor, used for the research of cancer. | [Brand name]
Calsed | [in vivo]
Amrubicin (SM-5887) (25 mg/kg, i.v.) exhibits significant antitumor activities against both SCLC tumors, Lu-24 and Lu-134, with T/C-values (comparing the mean tumor growth rates of the treated group with those of the control group for each day that the tumors are measured) at day 14 of 17% and 9%, respectively. Amrubicin (SM-5887) (25 mg/kg, i.v.) in combination with cisplatin and irinotecan significantly inhibits the growth of tumors compared to amrubicin alone in mice bearing LX-1 tumor cells. Amrubicin (SM-5887) alone or combined with tegafur and uracil also suppresses tumor growth in human cancer xenograft models[2]. | [IC 50]
Topoisomerase II | [References]
[1] Hayashi S, et al. Enhancement of radiosensitivity by topoisomerase II inhibitor, amrubicin and amrubicinol, in human lung adenocarcinoma A549 cells and kinetics of apoptosis and necrosis induction. Int J Mol Med. 2006 Nov;18(5):909-15. PMID:17016621
[2] Hanada M, et al. Amrubicin, a novel 9-aminoanthracycline, enhances the antitumor activity of chemotherapeutic agents against human cancer cells in vitro and in vivo. Cancer Sci. 2007 Mar;98(3):447-54. DOI:10.1111/j.1349-7006.2007.00404.x
[3] Hanada M, et al. Amrubicin induces apoptosis in human tumor cells mediated by the activation of caspase-3/7 preceding a loss of mitochondrial membrane potential. Cancer Sci. 2006 Dec;97(12):1396-403. Epub 2006 Sep 21. DOI:10.1111/j.1349-7006.2006.00318.x |
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