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Chemical Structure| 926927-61-9 Chemical Structure| 926927-61-9

Structure of Motolimod
CAS No.: 926927-61-9

Chemical Structure| 926927-61-9

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Motolimod is a Toll-like receptor 8 (TLR8) agonist with EC50 of 100 nM with immunostimulatory and antineoplastic activities.

Synonyms: VTX-2337; VTX-378

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Product Details of Motolimod

CAS No. :926927-61-9
Formula : C28H34N4O2
M.W : 458.60
SMILES Code : O=C(C1=CC2=CC=C(C3=CC=C(C(N4CCCC4)=O)C=C3)C=C2N=C(N)C1)N(CCC)CCC
Synonyms :
VTX-2337; VTX-378
MDL No. :MFCD28044318
InChI Key :QSPOQCXMGPDIHI-UHFFFAOYSA-N
Pubchem ID :16049404

Safety of Motolimod

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Motolimod

pyroptosis
TLR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK293 cells 0.1, 0.5, 5 µM 12 hours To investigate the effect of VTX-2337 on ERK activity in HEK293 cells, the results showed that VTX-2337 increased ERK luciferase activity at concentrations of 0.1 and 0.5 μM. PMC6279408
PBMC 250 nM 18 h Enhanced cetuximab-mediated ADCC, results showed that TLR8-stimulated PBMC significantly enhanced specific lysis of cetuximab-coated HNC cells PMC3720845
NK cells 250 nM 18 h TLR8-stimulated NK cells enhanced DC maturation markers CD80, CD83, and CD86 in the presence of cetuximab PMC3720845
PBMCs 0.1–2 μM 24 hours To evaluate the effect of VTX-2337 on cytokine secretion from PBMCs. Results showed that VTX-2337 significantly increased the secretion of IFNγ, TNFα, and IL-1β. PMC7810827
SQ20B HNSCC cells 2 µM 24 hours To evaluate the effect of VTX-2337 in combination with cetuximab on T cell and NK cell activation in a co-culture system of SQ20B HNSCC cells with PBMCs. Results showed that VTX-2337 significantly increased the activation of CD4+ and CD8+ T cells, but no enhanced effect was observed when combined with cetuximab. VTX-2337 alone did not increase NK cell activation, but when combined with cetuximab, it significantly increased NK cell activation. PMC7810827

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice BALB/c mice Intramuscular injection 2 μg/mouse Immunized on day 0 and day 7, blood collected on day 5 and day 12 To evaluate whether the combination of Motolimod with CL401 could enhance immune responses, results showed that Motolimod exhibited synergistic effects in enhancing immunogenicity PMC11880734
Mice Neuropathic pain model Intrathecal injection 100 ng Single injection To investigate the effect of VTX-2337 on neuropathic pain in mice, the results showed that VTX-2337 increased the mRNA expression of TNF-α, IL-1β, IL-6, and CCL2, indicating that VTX-2337 mediated inflammatory responses through TLR8. PMC6279408
Mice Trigeminal neuropathic pain model Intra-trigeminal ganglion injection 10, 50, 100 ng Single injection To study the effect of VTX-2337 on trigeminal neuropathic pain, results showed that VTX-2337 dose-dependently increased facial pain hypersensitivity. PMC8055805
Mice SCCVII/C3H, mEERL/C57Bl/6, TUBO-human EGFR/BALB/c Intraperitoneal injection 1 mg/kg Every other day for 2 weeks To evaluate the anti-tumor effect of VTX-2337 in different mouse models. Results showed that VTX-2337 significantly suppressed tumor growth in all three syngeneic mouse models and significantly prolonged the survival of cetuximab-treated mice. The combination of VTX-2337 with cetuximab significantly increased splenic lymphoid DCs and IFNγ+ CD4+ and tumor-specific CD8+ T cells. PMC7810827

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00688415 Advanced Solid Tumors|Lymphoma PHASE1 COMPLETED 2025-11-10 Mayo Clinic, Scottsdale, Arizo... More >>na, United States|Scottsdale Healthcare, Scottsdale, Arizona, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.90mL

2.18mL

1.09mL

21.81mL

4.36mL

2.18mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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