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Marizomib

CAS 号: 437742-34-2 (中文同义词:马里佐米)

所有产品仅用于科学研究,不得用于人体或动物实验。

目录号:HD00013

分子式:C15H20ClNO4

分子量:313.78

纯度:≥90%

长期储存条件:Store in a tight container at -20℃.

描述:Proteasome inhibitor

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Marizomib, also known as ML 858, NPI-0052 and Salinosporamide A, is a potent and selective 20S proteasome inhibitor from natural origin. Marizomib irreversibly inhibits proteasome to overcome compensatory hyperactivation in multiple myeloma and solid tumour patients. Marizomib activity as a single agent in malignant gliomas: ability to cross the blood-brain barrier. Marizomib exhibits prolonged inhibition, attenuated efflux, and greater cytotoxicity than its reversible analogs.

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参考文献

[1] Chauhan D, Singh A V, Ciccarelli B, et al. Combination of novel proteasome inhibitor NPI-0052 and lenalidomide trigger in vitro and in vivo synergistic cytotoxicity in multiple myeloma[J]. Blood, 2010, 115(4): 834-845.

[2] Singh A V, Palladino M A, Lloyd G K, et al. Pharmacodynamic and efficacy studies of the novel proteasome inhibitor NPI‐0052 (marizomib) in a human plasmacytoma xenograft murine model[J]. British journal of haematology, 2010, 149(4): 550-559.

[3] Das DS, Ray A, Song Y, Richardson P, Trikha M, Chauhan D, Anderson KC. Synergistic anti-myeloma activity of the proteasome inhibitor marizomib and the IMiD immunomodulatory drug pomalidomide. Br J Haematol. 2015 Dec;171(5):798-812. doi: 10.1111/bjh.13780. PubMed PMID: 26456076; PubMed Central PMCID: PMC4715649.

[4] Miller CP, Manton CA, Hale R, Debose L, Macherla VR, Potts BC, Palladino MA, Chandra J. Specific and prolonged proteasome inhibition dictates apoptosis induction by marizomib and its analogs. Chem Biol Interact. 2011 Oct 15;194(1):58-68. doi: 10.1016/j.cbi.2011.08.005. PubMed PMID: 21864512; PubMed Central PMCID: PMC3186881.

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