In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 100 nM (EC50)
Motolimod (VTX-2337) is a small molecule, selective Toll-like receptor (TLR) 8 agonist with EC50 value of 100 nM . 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 . 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 .
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) . Moreover, VTX-2337 (3 or 10 μM) induced mature IL-1β and IL-18 production through NLRP3 inflammasome activation in THP-1 cells .
In vivo: VTX-2337 (1 or 10 mg/kg, subcutaneous injection) induced IL-1β and IL-18 production in male cynomolgus monkeys .
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 .
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.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥15.7mg/mL in DMSO,insoluble in H2O, ≥45.8mg/mL in EtOH with ultrasonic and warming|
|Shipping Condition||Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.|
|General tips||For 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.|