首页 MAPK MNK ETC-206
ETC-206
编号 T15250    
CAS 1464151-33-4     分子式 C25H20N4O2     分子量 408.45
靶点: MNK1; MNK2;
ETC-206 is a selective inhibitor of MNK1 and MNK2 (IC50s: 64 nM and 86 nM).
选择批次  
规格 库存 单价 数量
5 mg 上海现货 1905.00
10 mg 上海现货 2925.00
25 mg 上海现货 5815.00
50 mg 上海现货 8365.00
100 mg 上海现货 12785.00
200 mg 上海现货 待询
500 mg 上海现货 待询
1 mL * 10 mM (in DMSO) 上海现货 2090.00
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生物活性

产品描述

ETC-206 is a selective inhibitor of MNK1 and MNK2 (IC50s: 64 nM and 86 nM).

靶点活性

MNK1,64 nM

MNK2,86 nM

体外活性

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). ETC-206 inhibits eIF4E phosphorylation in HeLa cell line (IC50: 321 nM). 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.

体内活性

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. 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 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 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.)).

化学信息

分子量

408.45

分子式

C25H20N4O2

CAS

1464151-33-4

溶解度

DMSO: 50 mg/mL (122.41 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.448 ml 12.241 ml 24.483 ml
5 mM 0.49 ml 2.448 ml 4.897 ml
10 mM 0.245 ml 1.224 ml 2.448 ml
50 mM 0.049 ml 0.245 ml 0.49 ml
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