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VTX-2337

Product Name
VTX-2337
CAS No.
926927-61-9
Chemical Name
VTX-2337
Synonyms
CS-1536;VTX 378;VTX-2337;Motolimod;Obicetrapib;VTX 2337;VTX2337;Motolimod(VTX-2337);VTX 2337;VTX2337;VTX-378;Motolimod, 10 mM in DMSO;2-amino-n,n-dipropyl-8-[4-(pyrrolidine-1-carbonyl)phenyl]-3h-1-benzazepine-4-carboxamide
CBNumber
CB42658210
Molecular Formula
C28H34N4O2
Formula Weight
458.6
MOL File
926927-61-9.mol
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VTX-2337 Property

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.
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
22952
Product name
Motolimod
Purity
≥98%
Packaging
1mg
Price
$33
Updated
2024/03/01
Cayman Chemical
Product number
22952
Product name
Motolimod
Purity
≥98%
Packaging
5mg
Price
$112
Updated
2024/03/01
Cayman Chemical
Product number
22952
Product name
Motolimod
Purity
≥98%
Packaging
10mg
Price
$208
Updated
2024/03/01
Cayman Chemical
Product number
22952
Product name
Motolimod
Purity
≥98%
Packaging
25mg
Price
$396
Updated
2024/03/01
AK Scientific
Product number
2129CW
Product name
Motolimod
Packaging
1mg
Price
$135
Updated
2021/12/16
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VTX-2337 Chemical Properties,Usage,Production

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

Raw materials

Preparation Products

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VTX-2337 Suppliers

China 116 India 1 United States 9 Global 126
Musechem
Tel
+1-800-259-7612
Fax
+1-800-259-7612
Email
info@musechem.com
Country
United States
ProdList
4660
Advantage
60
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32435
Advantage
58
InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
ProdList
6391
Advantage
58
Cckinase, Inc.
Tel
+1 (732)236-3202
Email
sales@cckinase.com
Country
United States
ProdList
2738
Advantage
58
BOC Sciences
Tel
+1-631-485-4226
Fax
1-631-614-7828
Email
inquiry@bocsci.com
Country
United States
ProdList
19552
Advantage
58
Aladdin Scientific
Tel
Email
tp@aladdinsci.com
Country
United States
ProdList
57505
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354;
Email
support@targetmol.com
Country
United States
ProdList
39035
Advantage
58
Focus Biomolecules
Tel
--
Fax
--
Email
sales@focusbiomolecules.com
Country
United States
ProdList
1284
Advantage
58
Cayman Chemical Company
Tel
--
Fax
--
Email
cayman@caymanchem.com
Country
United States
ProdList
6213
Advantage
81
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View Lastest Price from VTX-2337 manufacturers

Zhuozhou Wenxi import and Export Co., Ltd
Product
Motolimod 926927-61-9
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10
Zhuozhou Wenxi import and Export Co., Ltd
Product
Motolimod 926927-61-9
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-09

926927-61-9, VTX-2337Related Search:

Brefeldin A Troglitazone Adapalene 17-AAG CARBAMIC ACID, N-[2-[(R)-(3-CHLOROPHENYL)[(3R)-1-[[[(2S)-2-(METHYLAMINO)-3-[(3R)-TETRAHYDRO-2H-PYRAN-3-YL]PROPYL]AMINO]CARBONYL]-3-PIPERIDINYL]METHOXY]ETHYL]-, METHYL ESTER

  • 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
  • VTX 2337;VTX2337
  • CS-1536
  • 3H-1-Benzazepine-4-carboxamide, 2-amino-N,N-dipropyl-8-[4-(1-pyrrolidinylcarbonyl)phenyl]-
  • Motolimod, 10 mM in DMSO
  • 926927-61-9