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Motolimod | TLR8 agonist

CAS:
926927-61-9
Catalog Number:
10-4920
Activity:
TLR8 agonist/Cancer immunotherapy enhancer
Alternate Name:
VTX-2337
Chemical Name:
2-Amino-N,N-dipropyl-8-[4-(pyrrolidine-1-carbonyl)phenyl]-3H-1-benzapine-4-carboxamide
Molecular Weight:
458.61
Molecular Formula:
C28H34N4O2
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
Off-white or pale yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
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.
Shipping Code:
RT

Motolimod (926927-61-9) is a selective Toll-like receptor 8 (TLR8) agonist (EC50 = 100 nM). It stimulates the production of TNFα and IL-12 from monocytes and myeloid dendritic cells. Motolimod also stimulated IFNγ production from NK cells and increased their toxicity against K562 and ADCC by rituximab and trastuzumab.1,2 It induced apoptosis in monocytic myeloid-derived suppressor cells.3 Motolimod is being investigated in combination with other cancer immunotherapies.4,5 Motolimod has also been shown in induce secreted IL-1b and IL-8 via activation of the NLRP3 inflammasome.6

References/Citations:

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 P44
3) Rutman et al. (2015), Motolimod,a selective TLR8 agonist, induces apoptosis in monocytic myeloid-derived suppressor cells (M-MDSC); J. Immunother. Cancer. 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

Motolimod | TLR8 agonist is also available in the Cellular Metabolism Library.
CAS:
926927-61-9
Catalog Number:
10-4920
Activity:
TLR8 agonist/Cancer immunotherapy enhancer
Alternate Name:
VTX-2337
Chemical Name:
2-Amino-N,N-dipropyl-8-[4-(pyrrolidine-1-carbonyl)phenyl]-3H-1-benzapine-4-carboxamide
Molecular Weight:
458.61
Molecular Formula:
C28H34N4O2
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
Off-white or pale yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
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.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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