首页 MAPK MNK eFT508
eFT508
编号 T3468     别名: Tomivosertib
CAS 1849590-01-7     分子式 C17H20N6O2     分子量 340.39
靶点: MNK1; MNK2;
eFT508 is a potent, highly selective MNK1 and MNK2 inhibitor with IC50 value of 1-2 nM.
选择批次  
纯度 98.00%
规格 库存 单价 数量
1 mg 上海现货 679.00
5 mg 上海现货 1962.00
10 mg 上海现货 2912.00
1 mL * 10 mM (in DMSO) 上海现货 1962.00
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生物活性

产品描述

eFT508 is a potent, highly selective MNK1 and MNK2 inhibitor with IC50 value of 1-2 nM.

靶点活性

MNK1,2.4nM

MNK2,1nM

体外活性

eFT508 has a half-maximal inhibitory concentration (IC50) of 1-2 nM against both MNK isoforms in enzyme assays and inhibits the kinase through a reversible, ATP-competitive mechanism of action. Treatment of tumor cell lines with eFT508 leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50 = 2-16 nM). In a panel of ~50 hematological cancers, eFT508 shows anti-proliferative activity against multiple DLBCL cell lines. Sensitivity to eFT508 in TMD8, OCI-Ly3 and HBL1 DLBCL cell lines is associated with dose-dependent decreases in production of pro-inflammatory cytokines including TNFα, IL-6, IL-10 and CXCL10[1].

体内活性

eFT508 is well-tolerated and shows efficacy against MyD88-mutant DLBCL models in vivo. Significant anti-tumor activity of eFT508 is observed in the TMD8 and HBL-1 ABC-DLBCL models(subcutaneous human lymphoma xenograft models), both of which harbor activating MyD88 mutations[1].

细胞实验

TMD8 cells are treated with the indicated concentrations of eFT508 for 24 h. Cell lysates are subjected to m7-GTP Sepharose pull-down and bound proteins are analyzed by immunoblotting with the indicated antibodies. (Only for Reference)

细胞系: TMD8 cells

化学信息

分子量

340.39

分子式

C17H20N6O2

CAS

1849590-01-7

溶解度

DMSO: 11 mg/mL (32.3 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 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 2.938 ml 14.689 ml 29.378 ml
5 mM 0.588 ml 2.938 ml 5.876 ml
10 mM 0.294 ml 1.469 ml 2.938 ml
50 mM 0.059 ml 0.294 ml 0.588 ml
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