Art. -Nr.: HY-109049

Adavivint

(Synonyms: SM04690; Lorecivivint)

10 Cited Publications

Kundenbewertung

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.

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Reinheit: 98.85%
CAS. Nr.: 1467093-03-3
Formel: C₂₉H₂₄FN₇O
Molecular Weight:505.55

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Adavivint Chemical Structure

CAS. Nr.: 1467093-03-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (10)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

EC50: 19.5 nM (Wnt, SW480 cell)^[1]

Alle Wnt Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HT-22	IC₅₀	2.1 μM Compound: 23	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	[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.

In Vivo

Adavivint (0.3 μg) enhances cartilage repair and protection in the rat acute cruciate ligament tear and partial medial meniscectomy osteoarthritis (ACLT + pMMx OA) model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1467093-03-3
Appearance Solid
Molecular Weight 505.55
Formel C₂₉H₂₄FN₇O
Color Light yellow to gray
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
Synonyms

SM04690; Lorecivivint
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (10)

All Cell Proliferation/Viability AssayRT-PCRWBIF

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Journal Impact Factor

Chem Eng J

2024 Aug 1.

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.
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
University of Oklahoma

2024 May 10.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9780 mL

9.8902 mL

19.7804 mL

5 mM

0.3956 mL

1.9780 mL

3.9561 mL

10 mM

0.1978 mL

0.9890 mL

1.9780 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Deshmukh V, et al. A small-molecule inhibitor of the Wnt pathway (SM04690) as a potential disease modifying agent for the treatment of osteoarthritis of the knee. Osteoarthritis Cartilage. 2018 Jan;26(1):18-27. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Adavivint

10 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Adavivint

Alle Wnt Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Adavivint Related Classifications

HY-109049 Related Classifications