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Adavivint (SM04690) Wnt/beta-catenin inhibitor

Name: Adavivint (SM04690)
Brand: Selleck Chemicals
SKU: S8761
Availability: InStock
Rating: 5 (8 reviews)

Catalog No.S8761 Purity:98.13%

Adavivint (SM04690, Lorecivivint) is a potent and specific inhibitor of canonical Wnt signaling with an EC50 of 19.5 nM for inhibiting the TCF/LEF reporter. It is ∼150- to 500-fold more potent than the other known Wnt inhibitors across multiple cellular assays.

Chemical Structure

Molecular Weight: 505.55

Purity & Quality Control

Batch: S876101 DMSO]30 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 98.13%

98.13

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Signaling Pathway

Wnt/beta-catenin Signaling Pathway

Mechanism of Action

Targets

Wnt ^[1]

In vitro
In vitro	Adavivint (SM04690) induces a dose-dependent decrease in the expression of Wnt pathway genes (ASCL1, LEF1, TCF7L2, TCF7, C-262 MYC and AXIN2) in bone-marrow-derived hMSCs (CD29+, CD44+ CD166+ CD105+ CD45-). It also inhibits the expression of AXIN2, TCF7 and LEF1 in hMSCs and AXIN2 and LGR5 in IEC6 (intestinal stem cells sensitive to Wnt activation) when the Wnt pathway is selectively activated using either Wnt3a or a GSK3β inhibitor, CHIR-99021. This compound has minimal effects on the non-canonical Wnt pathway and the BMP pathway, and protects chondrocytes from catabolic breakdown in vitro^[1].
Cell Research	Cell lines	SW480 cells and hMSCs
	Concentrations	10, 30 and 100 nM
	Incubation Time	48 h
	Method	--

In Vivo
In vivo	Adavivint (SM04690) promotes cartilage growth and improves joint health in a rat model of knee osteoarthritis when administered via intra-articular injection. It decreases cartilage breakdown in vivo^[1].
Animal Research	Animal Models	Sprague-Dawley (SD) rats (12 weeks old, male)
	Dosages	0.3μg in 50μl
	Administration	intra-articular injection

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT03727022	Completed	Knee Osteoarthritis	Biosplice Therapeutics Inc.	November 28 2018	Phase 2
NCT03246399	Terminated	Degenerative Disc Disease	Biosplice Therapeutics Inc.	July 26 2017	Phase 1

References

https://pubmed.ncbi.nlm.nih.gov/28888902/

Chemical Information

Molecular Weight	505.55	Formula	C₂₉H₂₄FN₇O
CAS No.	1467093-03-3	SDF	--
Synonyms	Lorecivivint
Smiles	CC(C)CC(=O)NC1=CN=CC(=C1)C2=CC3=C(C=C2)NN=C3C4=NC5=C(N4)C=NC=C5C6=CC(=CC=C6)F

Storage and Stability

Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
			1 month-20°Cin solvent

In vitro
Batch:

DMSO : 30 mg/mL ( (59.34 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.750mg/ml (1.48mM)	Taking the 1 mL working solution as an example, add 50 μL of 15 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.180mg/ml (0.36mM)	Taking the 1 mL working solution as an example, add 50 μL of 3.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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