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Purity: ≥98%
Motolimod (also known as VTX-2337; VTX 378; VTX2337) is a novel, selective and potent small molecule agonist of the Toll-like receptor (TLR) 8 with immunostimulating/modulatory and anticancer effects. It activates TLR8 with EC50 of 100 nM, and displays > 50-fold selectivity over TLR7 and has potential immunostimulating and anticancer activities. Motolimod is currently under clinical development as an immunotherapy for multiple oncology indications such as 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.
| ln Vitro |
Motolimod (VTX-2337) selectively activates TLR8, out of all the studied TLRs (TLR2, 3, 4, 5, 7, 8, and 9). Motolimod increases TNFα (EC50=140±30 nM, based on 10 donors) and IL-12 (EC50=120±30 nM, based on 10 donors) production in peripheral blood monolayers. Motolimod has an EC50 value of 60 nM for inducing MIP-1β[1].
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| ln Vivo |
Motolimod (1 or 10 mg/kg) was given subcutaneously into the monkeys, and plasma was taken prior to the injection as well as six, twelve, twenty-four, and ninety-six hours later. Six hours after injection (10 mg/kg), mean plasma levels of IL-1β increased with 10 mg/kg Motolimod from a baseline level of 0.5 pg/mL to as high as 9.12±2.7 ng/mL (p<0.05, t-test). Additionally, circulating levels of IL-18 rose (p<0.05, t-test) from a baseline of approximately 1 pg/mL to 68.7±4.4 pg/mL. Since IL-6 is released in response to TLR8 activation but is not activated by NLRP3 inflammasome activation, IL-6 levels were observed. Additionally, IFNγ plasma levels were measured in response to Motolimod treatment-induced NK cell activation [2].
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| Additional Infomation |
Motolimod has been used in trials studying the treatment of Lymphoma, Tongue Cancer, Ovarian Cancer, Adult Solid Neoplasm, and Fallopian Tube Cancer, among others.
Motolimod is a small-molecule Toll-like receptor 8 (TLR8) agonist with potential immunostimulating and antineoplastic activities. Motolimod binds to TLR8, present in cutaneous dendritic cells, monocytes/macrophages, and mast cells, which may result in the activation of the central transcription factor nuclear factor-B, the secretion of proinflammatory cytokines and other mediators, and a Th1-weighted antitumoral cellular immune response. Primarily localized to endosomal membranes intracellularly, TLR8, like other TLRs, recognizes pathogen-associated molecular patterns (PAMPs) and plays a key role in the innate immune system. |
| Molecular Formula |
C28H34N4O2
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| Molecular Weight |
458.6
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| Exact Mass |
458.268
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| CAS # |
926927-61-9
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| Related CAS # |
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| PubChem CID |
16049404
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| Appearance |
Light yellow to brown solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
718.7±70.0 °C at 760 mmHg
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| Flash Point |
388.5±35.7 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.623
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| LogP |
2.71
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
771
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QSPOQCXMGPDIHI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H34N4O2/c1-3-13-31(14-4-2)28(34)24-17-23-12-11-22(18-25(23)30-26(29)19-24)20-7-9-21(10-8-20)27(33)32-15-5-6-16-32/h7-12,17-18H,3-6,13-16,19H2,1-2H3,(H2,29,30)
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| Chemical Name |
2-amino-N,N-dipropyl-8-[4-(pyrrolidine-1-carbonyl)phenyl]-3H-1-benzazepine-4-carboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1805 mL | 10.9027 mL | 21.8055 mL | |
| 5 mM | 0.4361 mL | 2.1805 mL | 4.3611 mL | |
| 10 mM | 0.2181 mL | 1.0903 mL | 2.1805 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 VTX-2337 is a selective and potent TLR8 agonist that induces TNFα and IL-12 production.Clin Cancer Res.2012 Jan 15;18(2):499-509. |
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 VTX-2337 selectively induces the production of TNFα and IL-12 and activates NF-κB phosphorylation in monocytes and mDCs, but not pDCs.Clin Cancer Res.2012 Jan 15;18(2):499-509. |
 VTX-2337 stimulates IFNγ production from NK cells.Clin Cancer Res.2012 Jan 15;18(2):499-509. |
 VTX-2337 enhances the NK cell lytic activity and augments rituximab- and trastuzumab-mediated ADCC.Clin Cancer Res.2012 Jan 15;18(2):499-509. |
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 VTX-2337 enhances ADCC in donors with different SNP on FcγR3A.Clin Cancer Res.2012 Jan 15;18(2):499-509. |
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