Adavivint
Based on 10 publication(s) in Google Scholar
Adavivint (SM04690; Lorecivivint) is a potent and selective inhibitor of canonical Wnt signaling, with an EC50 of 19.5 nM via a high-throughput TCF/LEF-reporter assay in SW480 colon cancer cells.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.85%
- No. CAS: 1467093-03-3
- Fòrmula: C29H24FN7O
- Peso molecular:505.55
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Adavivint
More- Chem Eng J. 2024 Aug 1.
- J Med Chem. 2023 Mar 23;66(6):4106-4130. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- Cell Oncol (Dordr). 2022 Dec;45(6):1401-1419. [Abstract]
- Eur J Pharm Biopharm. 2026 Mar:220:114980. [Abstract]
- Bone. 2022 May:158:116372. [Abstract]
- Mol Carcinog. 2023 Feb;62(2):160-173. [Abstract]
- Chem Biol Drug Des. 2024 Nov;104(5):e70012. [Abstract]
- Osteoarthr Cartil Open. 2023 May 12;5(3):100369. [Abstract]
- University of Oklahoma. 2024 May 10.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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RT-PCR
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RT-PCR
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WB
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IF
Actividad biológica
Descripciòn
IC50 & Target
EC50: 19.5 nM (Wnt, SW480 cell)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-22 | IC50 |
2.1 μM
Compound: 23
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Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
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[PMID: 36876904] |
In Vitro
Adavivint (SM04690) is a potent and selective inhibitor of Wnt signaling, with an EC50 of 19.5 nM via a high-throughput TCF/LEF-reporter assay in SW480 colon cancer cells, and shows no effect on SV40 luciferase reporter. Adavivint enhances aggregation of human mesenchymal stem cells (hMSCs) with an EC50 of 10 nM. Adavivint (30 nM) protects chondrocytes from catabolic breakdown in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1467093-03-3
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Appearance Solid
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Peso molecular 505.55
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Fòrmula C29H24FN7O
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Color Light yellow to gray
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SMILES
CC(C)CC(NC1=CC(C2=CC3=C(NN=C3C(N4)=NC5=C4C(C6=CC=CC(F)=C6)=CN=C5)C=C2)=CN=C1)=O
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Synonyms
SM04690; Lorecivivint
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (10)
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Journal Impact Factor
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Most Recent
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Adavivint purchased from MedChemExpress. Usage Cited in: Chem Eng J. 2024 Aug 1.
Using the CCK8 assay, the cytotoxic effects of different concentrations of SM04690 (10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM) on chondrocytes were examined.
Adavivint purchased from MedChemExpress. Usage Cited in: Chem Eng J. 2024 Aug 1.
After pretreatment with IL-1β, the gene expression of Aggrecan, COL2A1, ADAMTS5, and MMP 13 in chondrocytes was evaluated using various concentrations of SM04690 (30 nM, 0.1 μM, 0.3 μM).
Adavivint purchased from MedChemExpress. Usage Cited in: Chem Eng J. 2024 Aug 1.
After pretreatment with IL-1β and subsequent addition of SM04690 (30 nM) or KGN (40 μM), the gene expression of Aggrecan, COL2A1, ADAMTS5, and MMP 13 was evaluated.
Adavivint purchased from MedChemExpress. Usage Cited in: Chem Eng J. 2024 Aug 1.
After pretreatment with IL-1β and subsequent addition of SM04690 (30 nM) or KGN (40 μM), protein expression of Aggrecan, COL2A1, ADAMTS5, and MMP 13 was measured following the aforementioned treatments.
Adavivint purchased from MedChemExpress. Usage Cited in: Chem Eng J. 2024 Aug 1.
After pretreatment with IL-1β and subsequent addition of SM04690 (30 nM) or KGN (40 μM), immunofluorescence combined with DAPI staining was used to detect the expression of Collagen II.
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J Med Chem
Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases. [Abstract]2023 Mar 23;66(6):4106-4130. PMID: 36876904 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Cell Oncol (Dordr)
Novel preclinical gastroenteropancreatic neuroendocrine neoplasia models demonstrate the feasibility of mutation-based targeted therapy. [Abstract]2022 Dec;45(6):1401-1419. PMID: 36269546 -
Eur J Pharm Biopharm
Cationic liposome-mediated intra-articular delivery of lorecivivint for osteoarthritis treatment. [Abstract]2026 Mar:220:114980. PMID: 41519310 -
Bone
Intra-articular injection of a novel Wnt pathway inhibitor, SM04690, upregulates Wnt16 expression and reduces disease progression in temporomandibular joint osteoarthritis. [Abstract]2022 May:158:116372. PMID: 35218985 -
Mol Carcinog
PUS7 promotes the proliferation of colorectal cancer cells by directly stabilizing SIRT1 to activate the Wnt/β-catenin pathway. [Abstract]2023 Feb;62(2):160-173. PMID: 36222184 -
Chem Biol Drug Des
Mitotic Arrest Deficient 2 Like 1 Contributes to Colorectal Cancer Cell Migration, Invasion, and Oxaliplatin Resistance Through the Wnt/β-Catenin Pathway. [Abstract]2024 Nov;104(5):e70012. PMID: 39487106 -
Osteoarthr Cartil Open
Comparison of multiple synthetic chondroinductive factors in pellet culture against a TGF-β positive control. [Abstract]2023 May 12;5(3):100369. PMID: 37252634 -
Solvente y solubilidad
In Vitro:
DMSO : 25 mg/mL (49.45 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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Dual Luciferin reporter gene assay
Luciferin reporter gene assay is a reporting system to detect the activity of Firefly Luciferase using luciferin as a substrate, which is often used in the research of miRNA target gene verification and promoter transcriptive activity regulation. Dual luciferase usually refers to Firefly luciferase and Renilla luciferase.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9780 mL | 9.8902 mL | 19.7804 mL | 49.4511 mL |
| 5 mM | 0.3956 mL | 1.9780 mL | 3.9561 mL | 9.8902 mL | |
| 10 mM | 0.1978 mL | 0.9890 mL | 1.9780 mL | 4.9451 mL | |
| 15 mM | 0.1319 mL | 0.6593 mL | 1.3187 mL | 3.2967 mL | |
| 20 mM | 0.0989 mL | 0.4945 mL | 0.9890 mL | 2.4726 mL | |
| 25 mM | 0.0791 mL | 0.3956 mL | 0.7912 mL | 1.9780 mL | |
| 30 mM | 0.0659 mL | 0.3297 mL | 0.6593 mL | 1.6484 mL | |
| 40 mM | 0.0495 mL | 0.2473 mL | 0.4945 mL | 1.2363 mL |
Adavivint Related Classifications
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