eFT508

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

eFT508 (Tomivosertib) 是一种有效、高选择性、可逆、ATP 竞争性、口服生物可利用的 MNK1 和 MNK2 抑制剂，在酶测定中 IC50 为 1-2 nM。

eFT508 (Tomivosertib) is a?potent, highly selective, reversible, ATP-competitive, and orally bioavailable MNK1 and MNK2 inhibitor with IC50 of 1-2 nM in enzyme assays; dose-dependently reduces eIF4E phosphorylation at Serine 209 in tumor cell lines with IC50 of 2-16 nM; shows anti-proliferative activity against multiple DLBCL cell lines, decreases the production of pro-inflammatory cytokines including TNFα, IL-6, IL-10 and CXCL10; demonstrates significant anti-tumor activity in human lymphoma xenograft models which harbor activating MyD88 mutations.Blood Cancer Phase 2 Clinical(In Vitro):Tomivosertib (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, Tomivosertib shows anti-proliferative activity against multiple DLBCL cell lines. Sensitivity to Tomivosertib 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 Tomivosertib mechanism of action demonstrates that decreased TNFα production correlates with a 2-fold decrease in TNFα mRNA half-life. (In Vivo):Tomivosertib (eFT508) shows significant anti-tumor activity in the TMD8 and HBL-1 ABC-DLBCL models, both of which harbor activating MyD88 mutations. Besides, Tomivosertib combines effectively with components of R-CHOP and with novel targeted agents, including PCI-32765 and Venetoclax, in human lymphoma models.

Tomivosertib (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, Tomivosertib shows anti-proliferative activity against multiple DLBCL cell lines. Sensitivity to Tomivosertib 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 Tomivosertib mechanism of action demonstrates that decreased TNFα production correlates with a 2-fold decrease in TNFα mRNA half-life.

Tomivosertib (eFT508) shows significant anti-tumor activity in the TMD8 and HBL-1 ABC-DLBCL models, both of which harbor activating MyD88 mutations. Besides, Tomivosertib combines effectively with components of R-CHOP and with novel targeted agents, including PCI-32765 and Venetoclax, in human lymphoma models.

eFT 508 | Tomivosertib

MAPK/ERK Signaling

MNK

MNK1|MNK2

Cancer

Blood cancer

1849590-01-7

340.3797

C17H20N6O2

>98% (HPLC)

DMSO: 6 mg/mL (Need ultrasonic)

CC1=C2C(=O)NC3(N2C(=O)C(=C1)NC4=NC=NC(=C4)N)CCCCC3

Spiro[cyclohexane-1,3'(2'H)-imidazo[1,5-a]pyridine]-1',5'-dione, 6'-[(6-amino-4-pyrimidinyl)amino]-8'-methyl-

(-20℃)

With Ice Pack

≥ 2 years