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EFT508

CAT: 0013-GTR19163413-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19163413-01Size:200 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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.
CAS Number
1849590-01-7
Product Name Alternative
EFT 508 | Tomivosertib
Purity
>98% (HPLC)
Solubility
DMSO: 6 mg/mL (Need ultrasonic)
Smiles
CC1=C2C (=O) NC3 (N2C (=O) C (=C1) NC4=NC=NC (=C4) N) CCCCC3
Molecular Formula
C17H20N6O2
Molecular Weight
340.3797
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
Spiro[cyclohexane-1,3' (2'H) -imidazo[1,5-a]pyridine]-1',5'-dione, 6'-[ (6-amino-4-pyrimidinyl) amino]-8'-methyl-

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