1. MAPK/ERK Pathway
  2. MNK

eFT508 

Cat. No.: HY-100022 Purity: 99.49%
Data Sheet SDS Handling Instructions

eFT508 is a potent, highly selective, and orally bioavailable MNK1 and MNK2 inhibitor, with IC50 of 1-2 nM against both of the two isoforms.

For research use only. We do not sell to patients.
eFT508 Chemical Structure

eFT508 Chemical Structure

CAS No. : 1849590-01-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO $157 In-stock
1 mg $80 In-stock
5 mg $210 In-stock
10 mg $310 In-stock
50 mg $950 In-stock
100 mg $1350 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

eFT508 is a potent, highly selective, and orally bioavailable MNK1 and MNK2 inhibitor, with IC50 of 1-2 nM against both of the two isoforms.

IC50 & Target

IC50: 1-2 nM (MNK1), 1-2 nM (MNK2)[1]

In Vitro

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].

In Vivo

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].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.9379 mL 14.6895 mL 29.3789 mL
5 mM 0.5876 mL 2.9379 mL 5.8758 mL
10 mM 0.2938 mL 1.4689 mL 2.9379 mL
Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

340.38

Formula

C₁₇H₂₀N₆O₂

CAS No.

1849590-01-7

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 6 mg/mL (Need ultrasonic)

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.49%

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Product Name:
eFT508
Cat. No.:
HY-100022
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