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您的位置:首頁>>分析化學>>藥物分析標準品>>R5749 ROMIDEPSIN 128517-07-7
Cat. Number
R5749
Chemical Name
R5749 ROMIDEPSIN 128517-07-7
CAS Number
128517-07-7
Mol. Formula
C24H36N4O6S2
Mol. Weight
540.70
Qty 1
1mg
Qty 2
5mg
Appearance
White to off white powder
Application Notes
≥98%
Synonym
FK228, Istodax, Depsipeptide, FR901228, NSC630176
Solubility
DMSO 10 mg/mL (18.49 mM) Water Insoluble Ethanol Insoluble
Storage condition
-20°C
References

Romidepsin is a depsipeptide prodrug that inhibits histone deacetylases (HDACs). Romidepsin is currently in clinical trials as a potential treatment for T-cell lymphomas; it displays anticancer chemotherapeutic and antiviral activities. Romidepsin enhances in vitro and in vivo natural killer (NK) cell cytotoxicity by increasing MIC A/B (NK ligand) expression on tumor cells in leukemia and lymphoma models. Romidepsin also induces G0/G1 phase cell cycle arrest and apoptosis, upregulates expression of p21 and p53, downregulates expression of MMP2 and MMP9, and inhibits cell proliferation in non-small cell lung cancer (NSCLC) cells. In vitro, this product also induces HIV expression from infected CD4+ T cells, decreasing persistent latent HIV reservoirs.


References

Foss F, Coiffier B, Horwitz S, et al. Tolerability to romidepsin in patients with relapsed/refractory T-cell lymphoma. Biomark Res. 2014 Sep 8;2:16. PMID: 25279222.

Satwani P, Bavishi S, Saha A, et al. Upregulation of NKG2D ligands in acute lymphoblastic leukemia and non-Hodgkin lymphoma cells by romidepsin and enhanced in vitro and in vivo natural killer cell cytotoxicity. Cytotherapy. 2014 May 20. [Epub ahead of print]. PMID: 24856896.

Wei DG, Chiang V, Fyne E, et al. Histone deacetylase inhibitor romidepsin induces HIV expression in CD4 T cells from patients on suppressive antiretroviral therapy at concentrations achieved by clinical dosing. PLoS Pathog. 2014 Apr 10;10(4):e1004071. PMID: 24722454.

Karthik S, Sankar R, Varunkumar K, et al. Romidepsin induces cell cycle arrest, apoptosis, histone hyperacetylation and reduces matrix metalloproteinases 2 and 9 expression in bortezomib sensitized non-small cell lung cancer cells. Biomed Pharmacother. 2014 Apr;68(3):327-34. PMID: 24485799.

Ueda H, Nakajima H, Hori Y, et al. FR901228, a novel antitumor bicyclic depsipeptide produced by Chromobacterium violaceum No. 968. I. Taxonomy, fermentation, isolation, physico-chemical and biological properties, and antitumor activity. J Antibiot (Tokyo). 1994 Mar;47(3):301-10. PMID: 7513682.


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