- Motolimod
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- $31.00 / 1mg
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2026-05-27
- CAS:926927-61-9
- Min. Order:
- Purity: 99.66%
- Supply Ability: 10g
- VTX-2337
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- $0.00 / 25kg
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2026-04-24
- CAS:926927-61-9
- Min. Order: 1kg
- Purity: 98%
- Supply Ability: 1000kgs
- Motolimod
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- $15.00 / 1KG
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2021-07-13
- CAS:926927-61-9
- Min. Order: 1KG
- Purity: 99%+ HPLC
- Supply Ability: Monthly supply of 1 ton
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| | VTX-2337 Basic information |
| Product Name: | VTX-2337 | | Synonyms: | Obicetrapib;2-amino-n,n-dipropyl-8-[4-(pyrrolidine-1-carbonyl)phenyl]-3h-1-benzazepine-4-carboxamide;VTX-2337;VTX 378;Motolimod;2-amino-N,N-dipropyl-8-(4-(pyrrolidine-1-carbonyl)phenyl)-3H-benzo[b]azepine-4-carboxamide;Motolimod(VTX-2337);VTX 2337;VTX2337;VTX-378 | | CAS: | 926927-61-9 | | MF: | C28H34N4O2 | | MW: | 458.6 | | EINECS: | | | Product Categories: | | | Mol File: | 926927-61-9.mol |  |
| | VTX-2337 Chemical Properties |
| Boiling point | 718.7±70.0 °C(Predicted) | | density | 1.19±0.1 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | Soluble in DMSO (up to at least 25 mg/ml) | | form | solid | | pka | 2.47±0.40(Predicted) | | color | Off-white or pale yellow | | 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. | | 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/h7-12,17-19,30H,3-6,13-16,29H2,1-2H3 | | InChIKey | CQAGPRVMJDWWEA-UHFFFAOYSA-N | | SMILES | N4(CCCC4)C(=O)c1ccc(cc1)c2cc3c(cc2)C=C(C=C(N3)N)C(=O)N(CCC)CCC |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | VTX-2337 Usage And Synthesis |
| Description | Motolimod is an agonist of toll-like receptor 8 (TLR8). It increases the production of TNF-α and IL-12 in human peripheral blood mononuclear cells (PBMCs; EC50s = 140 and 120 nM, respectively), monocytes, and myeloid dendritic cells. Motolimod also increases IFN-γ production in natural killer (NK) cells and increases cytolysis in K562 NK cell-sensitive leukemia cells when used at concentrations of 167 and 500 nM for 48 hours. It increases plasma levels of a group of human cytokines, including IL-6, IL-12p70, TNF-α, MCP-1, and MIP-1β, in NOD-scid IL2rynull (NSG) mice reconstituted with human immune system (NSG-HIS) when administered at doses of 1.5 and 15 mg/m2. Motolimod, when used in combination with pegylated liposomal doxorubicin (PLD), reduces tumor growth and increases tumor infiltration of monocytes and T cells in an ovarian cancer NSG-HIS mouse model. | | Uses | Motolimod is an agonist of toll-like receptor 8 (TLR8) with potential immune-stimulating and antineoplastic properties. Motolimod is used in combination with PLD for the treatment of ovarian cancer. | | in vivo | Monkeys receive a subcutaneous injection of Motolimod (1 or 10 mg/kg), and plasma is collected predose, 6, 12, 24, and 96 h post-injection. For the 10 mg/kg dose, mean plasma levels of IL-1β increase from baseline levels of 0.5 pg/mL, up to 9.12±2.7 ng/mL (p<0.05, t-test) at 6 h post-administration of Motolimod (10 mg/kg). Circulating levels of IL-18 also increase from a baseline of ~ 1 pg/mL to 68.7±4.4 pg/mL (p<0.05, t-test) at 6 h in response to the Motolimod (VTX-2337) treatment (10 mg/kg). Levels of IL-6 are monitored, as this mediator is induced in response to TLR8 activation, but the release is independent of NLRP3 inflammasome activation. In addition, plasma levels of IFNγ are assessed as a measure of NK cell activation in response to Motolimod treatment[2]. | | IC 50 | TLR8 | | References | [1] HAILING LU. VTX-2337 is a novel TLR8 agonist that activates NK cells and augments ADCC.[J]. Clinical Cancer Research, 2012, 18 2: 499-509. DOI:10.1158/1078-0432.ccr-11-1625
[2] HAILING LU. TLR8 agonist VTX-2337 enhances NKG2D-mediated cytotoxicity of NK cells[J]. Journal for Immunotherapy of Cancer, 2013, 49 1: P44-P44. DOI:10.1186/2051-1426-1-s1-p44
[3] Z. J. RUTNAM. Motolimod, a selective TLR8 agonist induces apoptosis in monocytic myeloid-derived suppressor cells (M-MDSC)[J]. Journal for Immunotherapy of Cancer, 2015, 3 1: P296-P296. DOI:10.1186/2051-1426-3-s2-p296
[4] R. FERRIS. Active8: a randomized, 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]. Journal for Immunotherapy of Cancer, 2014, 2 1: P69-P69. DOI:10.1186/2051-1426-2-s3-p69
[5] B. MONK. Integrative Development of a TLR8 Agonist for Ovarian Cancer Chemoimmunotherapy[J]. Clinical Cancer Research, 2016, 23 1: 1955-1966. DOI:10.1158/1078-0432.ccr-16-1453
[6] G. DIETSCH. Coordinated Activation of Toll-Like Receptor8 (TLR8) and NLRP3 by the TLR8 Agonist, VTX-2337, Ignites Tumoricidal Natural Killer Cell Activity[J]. PLoS ONE, 2016, 11 1. DOI:10.1371/journal.pone.0148764 |
| | VTX-2337 Preparation Products And Raw materials |
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