型号:
产品价格:电议      采购度:1605      原产地:美洲
发布时间:2021/8/3 15:11:53 所属地区:上海 上海市
简要描述:
ETC-206 是一种选择性 MNK1 和 MNK2 抑制剂,IC50 分别为 64 nM 和 86 nM。
标签:etc-206
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CAS No. : 1464151-33-4
MCE 站:ETC-206
产品活性:ETC-206 是一种选择性 MNK1 和 MNK2 抑制剂,IC50 分别为 64 nM 和 86 nM。
研究领域:MAPK/ERK Pathway
作用靶点:MNK
In Vitro: ETC-206 inhibits eIF4E phosphorylation in HeLa cell line with an IC50 of 321 nM. The anti-proliferative effects of ETC-206 are assessed in vitro, using CellTiter-Glo viability assay against 25 hematological cancer cell lines including the K562 cell line that overexpresses eIF4E (K562 o/e eIF4E). The IC50s are 1.71 μM, 3.36 μM, 3.70 μM, 4.81 μM, 5.13 μM, 5.05 μM, 6.70 μM, 9.76 μM, and 48.8 μM for SU-DHL-6, GK-5, MC 116, P3HR-1, DOHH2, MPC-11, Ramos.2G6.4C10, AHH-1, and K562 o/e eIF4E cells, respectively.
In Vivo: The antitumor effect of ETC-206 is then assessed in a K562 e/o eIF4E mouse xenograft model after oral administration at 25, 50, or 100 mg/kg alone or in combination with a 2.5 mg/kg fixed dose of Dasatinib throughout the study. Dasatinib at 2.5 mg/kg elicits a tumor growth inhibition (TGI) of 88% with one tumor-free animal. In contrast, ETC-206 alone only yields a maximum TGI of 23% at the highest administered dose of 100 mg/kg, which does not impede tumor growth, and is similar to the nontreated animals. ETC-206 with 2.5 mg/kg of Dasatinib not only increases tumor growth inhibition in a dose-dependent manner but, more importantly leads to 2, 5, and 8 out of 8 tumor-free animals at 25, 50, and 100 mg/kg, respectively. The combination of ETC-206 and Dasatinib inhibits tumor growth at all tested doses, and no weight loss is recorded. Both the combination of ETC-206 and Dasatinib and, on the other hand, the dual MNK1/2 and BCR-ABL1 inhibitors prevent tumor growth in the same mouse xenograft model. ETC-206 has moderate terminal elimination half-life (t1/2=1.7 h, and 1.77 h for mouse (1 mg/kg, i.v.), mouse (5 mg/kg, p.o.)).
相关产品:Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | MAPK Compound Library | Anti-Cancer Compound Library | Oxygen Sensing Compound Library | CGP 57380 | Cercosporamide
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更新时间:2024/1/2 10:17:44
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