Adavivint (SM04690)

Catalog No.S8761 Synonyms: Lorecivivint

For research use only.

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.

Adavivint (SM04690) Chemical Structure

CAS No. 1467093-03-3

Selleck's Adavivint (SM04690) has been cited by 3 Publications

Purity & Quality Control

Choose Selective Wnt/beta-catenin Inhibitors

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Biological Activity

Description 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.
Targets
Wnt [1]
In vitro

Bone-marrow-derived hMSCs (CD29+, CD44+ CD166+ CD105+ CD45-), treated with SM04690, show a dose-dependent decrease in the expression of Wnt pathway genes (ASCL1, LEF1, TCF7L2, TCF7, C-262 MYC and AXIN2). M04690 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. SM04690 has minimal effects on the non-canonical Wnt pathway and the BMP pathway. SM04690 protects chondrocytes from catabolic breakdown in vitro[1].

In vivo

Intra-articular injection of SM04690 promotes cartilage growth and improves joint health in a rat model of knee osteoarthritis. It decreases cartilage breakdown in vivo[1].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: SW480 cells and hMSCs
  • Concentrations: 10, 30 and 100 nM
  • Incubation Time: 48 h
  • Method:

    --

Animal Research:

[1]

  • Animal Models: Sprague-Dawley (SD) rats (12 weeks old, male)
  • Dosages: 0.3μg in 50μl
  • Administration: intra-articular injection

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 505.55
Formula

C29H24FN7O

CAS No. 1467093-03-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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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.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03727022 Completed Drug: Placebo|Drug: SM04690 Knee Osteoarthritis Biosplice Therapeutics Inc. November 28 2018 Phase 2
NCT03246399 Terminated Drug: SM04690 Degenerative Disc Disease Biosplice Therapeutics Inc. July 26 2017 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-11-29)

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

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