产品信息
抗原名称
MNK2 ,MNK1
商品描述
eFT508 is a potent, highly selective MNK1 and MNK2 inhibitor with IC50 value of 1-2 nM.
分子量
340.38
纯度
>98%
可溶性
DMSO : 6 mg/mL (17.63 mM; Need ultrasonic)
外观
Powder
In vitro(体外研究)
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.
In vivo(体内研究)
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.
背景
别名
eFT 508；eFT-508；Tomivosertib
分子式
C17H20N6O2
CAS号
1849590-01-7
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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