Tomivosertib |
Catalog No.GC19131 |
Tomivosertib(eFT508)은 두 동형에 대해 IC50이 1-2nM인 강력하고 고도로 선택적인 경구 활성 MNK1 및 MNK2 억제제입니다. Tomivosertib(eFT508) 치료는 종양 세포주에서 세린 209(IC50=2-16nM)에서 eIF4E 인산화의 용량 의존적 감소를 유도합니다. Tomivosertib(eFT508)은 또한 PD-L1 단백질 풍부도를 극적으로 하향 조절합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1849590-01-7
Sample solution is provided at 25 µL, 10mM.
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;
Average Rating: 5
(Based on Reviews and 23 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *