eFT508CAS号: 1849590-01-7分子式: C17H20N6O2分子量: 340.38描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
eFT508 is a potent, highly selective MNK1 and MNK2 inhibitor with IC50 value of 1-2 nM. |
纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
eFT 508;eFT-508;Tomivosertib
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外观 |
Powder
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可溶性/溶解性 |
DMSO : 6 mg/mL (17.63 mM; Need ultrasonic)
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生物活性 | |
靶点 |
MNK2 ,MNK1
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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.
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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.
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分子结构图