Motolimod (VTX-2337)

Catalog No.S7161

Motolimod (VTX-2337) Chemical Structure

Molecular Weight(MW): 458.6

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

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Biological Activity

Description Motolimod (VTX-2337) is a selective and potent Toll-like receptor (TLR) 8 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

Kinase Assay:[1]
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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]
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  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 55 mg/mL warmed (119.93 mM)
Ethanol 15 mg/mL (32.7 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 458.6
Formula

C28H34N4O2

CAS No. 926927-61-9
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02650635 Active, not recruiting Colorectal Adenocarcinoma|Metastatic Pancreatic Adenocarcinoma|Recurrent Breast Carcinoma|Recurrent Colorectal Carcinoma|Recurrent Melanoma of the Skin|Recurrent Non-Small Cell Lung Carcinoma|Recurrent Pancreatic Carcinoma|Recurrent Renal Cell Carcinoma|Solid Neoplasm|Stage IV Breast Cancer|Stage IV Non-Small Cell Lung Cancer|Stage IV Renal Cell Cancer|Stage IV Skin Melanoma|Stage IVA Colorectal Cancer|Stage IVA Pancreatic Cancer|Stage IVB Colorectal Cancer|Stage IVB Pancreatic Cancer Mayo Clinic|National Cancer Institute (NCI) February 2016 Phase 1
NCT02124850 Recruiting Squamous Cell Carcinoma of the Head and Neck VentiRx Pharmaceuticals Inc. September 2014 Phase 1
NCT01836029 Active, not recruiting Carcinoma, Squamous Cell of Head and Neck VentiRx Pharmaceuticals Inc. July 2013 Phase 2
NCT01666444 Active, not recruiting Epithelial Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Cancer VentiRx Pharmaceuticals Inc.|Gynecologic Oncology Group October 2012 Phase 2
NCT01289210 Terminated Low Grade B Cell Lymphoma VentiRx Pharmaceuticals Inc.|Stanford University July 2011 Phase 1|Phase 2
NCT01334177 Completed Metastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma|Recurrent Metastatic Squamous Neck Cancer With Occult Primary|Recurrent Salivary Gland Cancer|Recurrent Squamous Cell Carcinoma of the Hypopharynx|Recurrent Squamous Cell Carcinoma of the Larynx|Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity|Recurrent Squamous Cell Carcinoma of the Nasopharynx|Recurrent Squamous Cell Carcinoma of the Oropharynx|Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity|Recurrent Verrucous Carcinoma of the Larynx|Recurrent Verrucous Carcinoma of the Oral Cavity|Salivary Gland Squamous Cell Carcinoma|Stage III Salivary Gland Cancer|Stage III Squamous Cell Carcinoma of the Hypopharynx|Stage III Squamous Cell Carcinoma of the Larynx|Stage III Squamous Cell Carcinoma of the Lip and Oral Cavity|Stage III Squamous Cell Carcinoma of the Nasopharynx|Stage III Squamous Cell Carcinoma of the Oropharynx|Stage III Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity|Stage III Verrucous Carcinoma of the Larynx|Stage III Verrucous Carcinoma of the Oral Cavity|Stage IV Salivary Gland Cancer|Stage IVA Squamous Cell Carcinoma of the Larynx|Stage IVA Squamous Cell Carcinoma of the Lip and Oral Cavity|Stage IVA Squamous Cell Carcinoma of the Oropharynx|Stage IVA Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity|Stage IVA Verrucous Carcinoma of the Larynx|Stage IVA Verrucous Carcinoma of the Oral Cavity|Stage IVB Squamous Cell Carcinoma of the Larynx|Stage IVB Squamous Cell Carcinoma of the Lip and Oral Cavity|Stage IVB Squamous Cell Carcinoma of the Oropharynx|Stage IVB Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity|Stage IVB Verrucous Carcinoma of the Larynx|Stage IVB Verrucous Carcinoma of the Oral Cavity|Stage IVC Squamous Cell Carcinoma of the Larynx|Stage IVC Squamous Cell Carcinoma of the Lip and Oral Cavity|Stage IVC Squamous Cell Carcinoma of the Oropharynx|Stage IVC Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity|Stage IVC Verrucous Carcinoma of the Larynx|Stage IVC Verrucous Carcinoma of the Oral Cavity|Tongue Cancer University of Washington|National Cancer Institute (NCI) June 2011 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID