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Tomivosertib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tomivosertib图片
CAS NO:1849590-01-7
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Tomivosertib (eFT508) 是一种有效的、高度选择性的、具有口服活性的 MNK1 和 MNK2 抑制剂,对两种亚型的 IC50 为 1-2 nM。 Tomivosertib (eFT508) 治疗导致肿瘤细胞系中丝氨酸 209 (IC50=2-16 nM) 的 eIF4E 磷酸化呈剂量依赖性降低。 Tomivosertib (eFT508) 也显着下调 PD-L1 蛋白丰度。
Cas No.1849590-01-7
别名6'-[(6-氨基-4-嘧啶基)氨基]-8'-甲基螺[环己烷-1,3'(2'H)-咪唑并[1,5-A]吡啶]-1',5'-二酮,eFT508
Canonical SMILESO=C(C1=C(C)C=C(NC2=NC=NC(N)=C2)C(N13)=O)NC43CCCCC4
分子式C17H20N6O2
分子量340.38
溶解度DMSO : 4.35 mg/mL (12.78 mM);Water :< 0.1 mg/mL (insoluble)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

eFT508 is a potent, highly selective, and orally bioavailable MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms.

eFT508 reduces eIF4E phosphorylation dose-dependently at serine 209 (IC50=2-16 nM) in tumor cell lines. In a panel of appr 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. Further evaluation eFT508 mechanism of action demonstrates that decreased TNFα production correlates with a 2-fold decrease in TNFα mRNA half-life[1].

eFT508 shows significant anti-tumor activity in the TMD8 and HBL-1 ABC-DLBCL models, both of which harbor activating MyD88 mutations. Besides, eFT508 combines effectively with components of R-CHOP and with novel targeted agents, including ibrutinib and venetoclax, in human lymphoma models[1].

References:
[1]. Kevin R. Webster, et al. eFT508, a Potent and Selective Mitogen-Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 Inhibitor, Is Efficacious in Preclinical Models of Diffuse Large B-Cell Lymphoma (DLBCL). Blood 2015 126:1554;