Motolimod (VTX-2337)

Catalog No.S7161

For research use only.

Motolimod (VTX-2337) is a selective and potent Toll-like receptor 8 (TLR8) agonist with EC50 of 100 nM, > 50-fold selectivity over TLR7. Phase 2.

Motolimod (VTX-2337) Chemical Structure

CAS No. 926927-61-9

Selleck's Motolimod (VTX-2337) has been cited by 9 Publications

Purity & Quality Control

Choose Selective TLR Inhibitors

Biological Activity

Description Motolimod (VTX-2337) is a selective and potent Toll-like receptor 8 (TLR8) agonist with EC50 of 100 nM, > 50-fold selectivity over TLR7. Phase 2.
Targets
TLR8 [1]
100 nM(EC50)
In vitro

VTX-2337 stimulates the production of both TNFα with EC50 of 140 nM and IL-12 with EC50 of 120 nM in PBMCs. In monocytes and mDCs, VTX-2337 selectively induces the production of TNFα and IL-12 via NF-κB activation. VTX-2337 also stimulates IFNγ production from NK cells, augments the lytic function of NK cells and enhances ADCC. [1]

In vivo In an ovarian cancer mouse model, TX-2337 enhances the effect of pegylated liposomal doxorubicin (PLD). [2]

Protocol (from reference)

Kinase Assay:[1]
  • Activity assay:

    The activity of specific TLR agonists is assessed using the secretory embryonic alkaline phosphatase (SEAP) reporter gene that is linked to NF-κB activation in response to TLR stimulation. Measurement of SEAP activity using the Quanti-blue substrate (InvivoGen) after TLR agonist treatment is carried out.

Cell Research:[1]
  • Cell lines: PBMCs or purified NK cells
  • Concentrations: ~500 nM
  • Incubation Time: 48 h
  • Method: PBMCs or purified NK cells are prepared as previously described, and the purity of NK cells was approximately 99%. NK cell–mediated cytotoxicity is assessed by Calcein AM release from labeled target cells. In brief, PBMCs or purified NK cells are cultured for 48 hours in RPMI medium in the presence of VTX-2337 (167 or 500 nmol/L) before incubation with target cells.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 458.6
Formula

C28H34N4O2

CAS No. 926927-61-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCN(CCC)C(=O)C1=CC2=C(C=C(C=C2)C3=CC=C(C=C3)C(=O)N4CCCC4)N=C(C1)N

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03906526 Completed Drug: VTX-2337|Drug: Nivolumab Carcinoma Squamous Cell Celgene July 3 2019 Phase 1
NCT01289210 Terminated Drug: VTX-2337 plus radiotherapy Low Grade B Cell Lymphoma Celgene|Stanford University July 2011 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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