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              S26163

              Tosedostat (CHR2797)

              MedMol 96%
              • 英文名:
              • (S)-cyclopentyl 2-((R)-2-((S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl)-4-methylpentanamido)-2-phenylacetate
              • 別名:
              • 托舍多特;CHR2797; CHR-2797; CHR 2797; Tosedostat.
              • CAS號:
              • 238750-77-1
              • 分子式:
              • C21H30N2O6
              • 分子量:
              • 406.47
              • 核磁/質譜:
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              參考文獻

              質檢證書(COA)

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              • 產品描述:

                  Tosedostat is a proprietary orally bioavailable inhibitor of the M1 family of aminopeptidases with potential antineoplastic activity. Tosedostat is converted intracellularly into a poorly membrane-permeable active metabolite (CHR-79888) which inhibits the M1 family of aminopeptidases, particularly puromycin-sensitive aminopeptidase (PuSA), and leukotriene A4 (LTA4) hydrolase; inhibition of these aminopeptidases in tumor cells may result in amino acid deprivation, inhibition of protein synthesis due to a decrease in the intracellular free amino acid pool, an increase in the level of the proapoptotic protein Noxa, and cell death.

              • 靶點: M1-aminopeptidase
              • 體外研究: In HL-60 cells, the treatmentwith Tosedostat (CHR-2797) results in an increase in the secretion of Stanniocalcin 2 (STC2) protein into the growth medium. After 2 h treatment with Tosedostat (60 nM), increases in SLC7A11 expression are detectable. The for by Tosedostat inhibits the proliferation of U-937 and HuT 78 cell lines (IC50s: 10 nM; >10 μM). Tosedostat treatment increases expression of amino acid deprivation response (AADR) genes in U-937 cells but not in HuT 78 cells. By 24 h with Tosedostat (0.01 μM) the mean MCA production is reduced to 77.8% of the untreated control cells; similarly the MCA production is reduced to 51.3% with 1 μM, 38.5% with 5 μM, and 35.3% with 10 μM Tosedostat.
              • 體內研究: In vivo in rodent cancer models, Tosedostat (CHR-2797) has anticancer activity, and a dose-response relationship has been shown in two models. The effect of Tosedostat is less apparent when the tumor burden is higher before therapy.
              • 細胞實驗: Tosedostat (CHR-2797) is stored at -20°C as a 10 mM stock in dimethyl sulfoxide (DMSO), and diluted with RPMI culture medium prior to use. Leukemic cells are washed and suspended in phosphate buffered saline (PBS). 100 μL of cell suspension (1×105 cells/mL) is mixed with 100 μL of Tosedostat (CHR-2797) (0.01 to 10 μM) and 200 μM L-alanine 4-methyl-coumaryl-7-amide (ala-MCA) in a 96 well plate in duplicate. The aminopeptidase activity is measured by detecting the fluorescent 7-amino-4-methylcoumarin (MCA) liberated from the cleavage of ala-MCA by cellular aminopeptidases (excitation 355 nm, emission 460 nm).
              • 動物實驗: A breeding colony of NOD/SCID IL2R gammanull mice are used in this study. The mice are inoculated subcutaneously in the right flank with 2×106 H929 myeloma cells in 50 μL RPMI-1640 and 50 μL MatrigelTM Basement Membrane Matrix Growth Factor Reduced. The mice are assigned into the following four treatment groups (10 animals per group): no treatment, Tosedostat 75 mg/kg, CHR-3996 30 mg/kg, and Tosedostat 75 mg/kg with concomitant CHR-3996 30 mg/kg. Tosedostat is administered daily by intra-peritoneal injection beginning four days after the tumour cells are inoculated. Caliper measurements of the longest perpendicular tumour diameters (length) and width are performed every other day to estimate the tumour volume.
              • 參考文獻:
                1. Aminopeptidase inhibition by the novel agent CHR-2797 (tosedostat) for the therapy of acute myeloid leukemia By Jenkins, Christopher; Hewamana, Saman; Krige, David; Pepper, Chris; Burnett, Alan From Leukemia Research (2011), 35(5), 677-681.
                2. Phase I/II clinical study of tosedostat, an inhibitor of aminopeptidases, in patients with acute myeloid leukemia and myelodysplasia By Loewenberg, Bob; Morgan, Gareth; Ossenkoppele, Gert I.; Burnett, Alan K.; Zachee, Pierre; Duehrsen, Ulrich; Dierickx, Daan; Mueller-Tidow, Carsten; Sonneveld, Pieter; Krug, Utz; et al From Journal of Clinical Oncology (2010), 28(28), 4333-4338.
                3. A Phase Ib dose-escalation study to evaluate safety and tolerability of the addition of the aminopeptidase inhibitor tosedostat (CHR-2797) to paclitaxel in patients with advanced solid tumours By van Herpen, C. M. L.; Eskens, F. A. L. M.; de Jonge, M.; Desar, I.; Hooftman, L.; Bone, E. A.; Timmer-Bonte, J. N. H.; Verweij, J. From British Journal of Cancer (2010), 103(9), 1362-1368.
                4. Quinazoline derivatives and methods of treatment By Tung, Roger From U.S. Pat. Appl. Publ. (2010), US 20100260674 A1 20101014.
                5. Surface topographies for non-toxic bioadhesion control By Brennan, Anthony B.; Long, Christopher James; Bagan, Joseph W.; Schumacher, James Frederick; Spiecker, Mark M. From U.S. Pat. Appl. Publ. (2010), US 20100226943 A1 20100909.
                6. Starving to succeed By Davenport, Emma L.; Aronson, Lauren I.; Davies, Faith E. From Autophagy (2009), 5(7), 1052-1054.
                7.
              • 溶解度: DMSO  :  15  mg/mL  
                母液保存:分裝凍存,避免反復凍融;-20℃,1個月;-80℃,6個月(稀釋后溶液溫度低保存可能會析出,盡量現用現配)
                細胞實驗:先用DMSO溶解:再用培養基進行稀釋,稀釋過程建議分段進行,避免濃度變化過快導致化合物析出。若稀釋過程中出現化合物析出的情況,  可采用超聲的方法使其復溶。在稀釋時要確保工作液中  DMSO  的終濃度盡量在0.1%以下,最高不要超過0.5%,并設置相應濃度的DMSO對照組。
                動物實驗:先用DMSO溶解:再用水或者生理鹽水等去稀釋,稀釋過程建議分段進行,避免濃度變化過快導致化合物析出。若稀釋過程中出現化合物析出的情況,  可采用超聲的方法使其復溶??梢酝ㄟ^添加助溶劑來幫助溶解,比如植物油、Tween80、甘油、羧甲基纖維素鈉和PEG400等。具體方式請參考文獻。懸濁液可用于口服和腹腔注射,不會影響產品活性。
              • 保存條件: -20℃
              • 配置溶液濃度參考:
                1mg 5mg 10mg
                1 mM 2.46 ml 12.301 ml 24.602 ml
                5 mM 0.492 ml 2.46 ml 4.92 ml
                10 mM 0.246 ml 1.23 ml 2.46 ml
                50 mM 0.049 ml 0.246 ml 0.492 ml
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