Supplier Related Products Identification Chemical Properties Hazard Information
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926927-61-9

Supplier Related Products Identification Chemical Properties Hazard Information

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Identification

Name
VTX-2337
CAS
926927-61-9
Synonyms
VTX 378
CS-1536
VTX-2337
Motolimod
Obicetrapib
VTX 2337;VTX2337
Motolimod(VTX-2337)
VTX 2337;VTX2337;VTX-378
2-amino-n,n-dipropyl-8-[4-(pyrrolidine-1-carbonyl)phenyl]-3h-1-benzazepine-4-carboxamide
2-amino-N,N-dipropyl-8-(4-(pyrrolidine-1-carbonyl)phenyl)-3H-benzo[b]azepine-4-carboxamide
3H-1-Benzazepine-4-carboxamide, 2-amino-N,N-dipropyl-8-[4-(1-pyrrolidinylcarbonyl)phenyl]-
Molecular Formula
C28H34N4O2
MOL File
926927-61-9.mol
Molecular Weight
458.6

Chemical Properties

Boiling point 
718.7±70.0 °C(Predicted)
density 
1.19±0.1 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
Soluble in DMSO (up to at least 25 mg/ml)
form 
solid
pka
2.47±0.40(Predicted)
color 
Off-white or pale yellow
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Hazard Information

Description
Motolimod is an agonist of toll-like receptor 8 (TLR8). It increases the production of TNF-α and IL-12 in human peripheral blood mononuclear cells (PBMCs; EC50s = 140 and 120 nM, respectively), monocytes, and myeloid dendritic cells. Motolimod also increases IFN-γ production in natural killer (NK) cells and increases cytolysis in K562 NK cell-sensitive leukemia cells when used at concentrations of 167 and 500 nM for 48 hours. It increases plasma levels of a group of human cytokines, including IL-6, IL-12p70, TNF-α, MCP-1, and MIP-1β, in NOD-scid IL2rynull (NSG) mice reconstituted with human immune system (NSG-HIS) when administered at doses of 1.5 and 15 mg/m2. Motolimod, when used in combination with pegylated liposomal doxorubicin (PLD), reduces tumor growth and increases tumor infiltration of monocytes and T cells in an ovarian cancer NSG-HIS mouse model.
Uses
Motolimod is an agonist of toll-like receptor 8 (TLR8) with potential immune-stimulating and antineoplastic properties. Motolimod is used in combination with PLD for the treatment of ovarian cancer.
References
1) Lu?et al.?(2012),?VTX-2337 is a Novel TLR8 Agonist That Activates NK Cells and Augments ADCC;?Clin. Cancer Res.?18?499 2) Lu?et al.?(2013),?TLR8 agonist VTX-2337 enhances NKG2D-mediated cytotoxicity of NK cells;?J. Immunother. Cancer?1?P44 3) Rutman?et al.?(2015),?Motolimod,a selective TLR8 agonist, induces apoptosis in monocytic myeloid-derived suppressor cells (M-MDSC);?J. Immunother. Cancer.?3?P296 4) Ferris?et al.?(2014),?Active8: a random, double-blind, placebo-controlled study of chemotherapy plus cetuximab in combination with TLR8 agonist VTX-2337 in patients with recurrent or metastatic squamous cell carcinoma of the head and neck (SCCHN);?J. Immunother. Cancer?2P69 5) Monk?et al.?(2017),?Integrative Development of a TLR8 Agonist for Ovarian Cancer Chemo-Immunotherapy;?Clin. Cancer Res.?23?1955 6) Dietsch?et al.?(2016),?Coordinated Activation of Toll-Like Receptor8 (TLR8) and NLRP3 by the TLR8 Agonist, VTX-2337, Ignites Tumoricidal Natural Killer Cell Activity;?PLoS One?11?e0148764
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