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Motolimod (VTX-2337)

Catalog No.
B5996
TLR8 agonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$190.00
In stock
5mg
$130.00
In stock
25mg
$380.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Target: TLR8

IC50: 100 nM (EC50)

Motolimod (VTX-2337) is a small molecule, selective Toll-like receptor (TLR) 8 agonist with EC50 value of 100 nM [1]. VTX-2337 is currently in clinical development as an immunotherapy for multiple oncology indications, including ovarian cancer and squamous cell carcinoma of the head and neck [2]. TLR8 is located in the endosome where it functions in the recognition of foreign nucleic acids from intracellular pathogens. TLR8 has emerged as a potential target for anticancer immunotherapies [1].

In vitro: VTX-2337 (800 nmol/L) activated NK cells, leading to increased TNFα and IL-12, IFNγ production and VTX-2337 (167 or 500 nmol/L) augmented rituximab- and trastuzumab-mediated antibody-dependent cell-mediated cytotoxicity (ADCC) [1]. Moreover, VTX-2337 (3 or 10 μM) induced mature IL-1β and IL-18 production through NLRP3 inflammasome activation in THP-1 cells [2].

In vivo: VTX-2337 (1 or 10 mg/kg, subcutaneous injection) induced IL-1β and IL-18 production in male cynomolgus monkeys [2].

Clinical trial: In a phase I dose-finding study, VTX-2337 (0.1–3.9 mg/m2, subcutaneous administration) was well tolerated and active with a predictable pharmacologic profile in adult subjects with advanced solid tumors or lymphoma [3].

References:
1.  Lu H, Dietsch GN, Matthews MA, Yang Y, Ghanekar S, Inokuma M, et al. VTX-2337 is a novel TLR8 agonist that activates NK cells and augments ADCC. Clin Cancer Res. 2012;18(2):499-509.
2.  Dietsch GN, Lu H, Yang Y, Morishima C, Chow LQ, Disis ML, et al. Coordinated Activation of Toll-Like Receptor8 (TLR8) and NLRP3 by the TLR8 Agonist, VTX-2337, Ignites Tumoricidal Natural Killer Cell Activity. PLoS One. 2016;11(2):e0148764.
3.  Northfelt DW, Ramanathan RK, Cohen PA, Von Hoff DD, Weiss GJ, Dietsch GN, et al. A phase I dose-finding study of the novel Toll-like receptor 8 agonist VTX-2337 in adult subjects with advanced solid tumors or lymphoma. Clin Cancer Res. 2014;20(14):3683-91.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt458.6
Cas No.926927-61-9
FormulaC28H34N4O2
Solubility≥15.7mg/mL in DMSO,insoluble in H2O, ≥45.8mg/mL in EtOH with ultrasonic and warming
Chemical Name2-imino-N,N-dipropyl-8-(4-(pyrrolidine-1-carbonyl)phenyl)-2,3-dihydro-1H-benzo[b]azepine-4-carboxamide
SDFDownload SDF
Canonical SMILESCCCN(C(C(CC1=N)=CC2=C(N1)C=C(C3=CC=C(C(N4CCCC4)=O)C=C3)C=C2)=O)CCC
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control