Adavivint


Catalog No. size PriceQuantity
M6927-2 2mg solid $100
M6927-10 10mg solid $411

Description

Cas:1467093-03-3

Product Information:

Adavivint, also known as SM04690, is a small-molecule inhibitor of the Wnt pathway which is being investigated as a potential disease modifying agent for the treatment of osteoarthritis of the knee.

 

Chemical Formula: C29H24FN7O

Exact Mass: 505.2026

 

Molecular Weight: 505.56

 

Elemental Analysis: C, 68.90; H, 4.79; F, 3.76; N, 19.39; O, 3.16

 

Related CAS #: 1467093-03-3 (free base)    

 

Synonym:

 

SM-04690

 

Chemical Name: 

N-(5-(3-(7-(3-Fluorophenyl)-3H-imidazo(4,5-C)pyridin-2-yl)-1H-indazol-5- yl)-pyridin-3-yl)-3-methylbutanamide

 

InChi Key:

AQDWDWAYVBQMAM-UHFFFAOYSA-N

 

InChi Code: 

1S/C29H24FN7O/c1-16(2)8-26(38)33-21-10-19(12-31-13-21)17-6-7-24-22(11-17)28(37-36-24)29-34-25-15-32-14-23(27(25)35-29)18-4-3-5-20(30)9-18/h3-7,9-16H,8H2,1-2H3,(H,33,38)(H,34,35)(H,36,37)

 

Smiles Code:

CC(C)CC(=O)Nc1cncc(c1)c2ccc3[nH]nc(c4nc5c(cncc5[nH]4)c6cccc(F)c6)c3c2

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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.

 

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.

 

 

References:

 

  1. Deshmukh V, Hu H, Barroga C, Bossard C, Kc S, Dellamary L, Stewart J, Chiu K, Ibanez M, Pedraza M, Seo T, Do L, Cho S, Cahiwat J, Tam B, Tambiah JRS, Hood J, Lane NE, Yazici Y. 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. doi: 10.1016/j.joca.2017.08.015. Epub 2017 Sep 6. PubMed PMID: 28888902.

 

  1. Yazici Y, McAlindon TE, Fleischmann R, Gibofsky A, Lane NE, Kivitz AJ, Skrepnik N, Armas E, Swearingen CJ, DiFrancesco A, Tambiah JRS, Hood J, Hochberg MC. A novel Wnt pathway inhibitor, SM04690, for the treatment of moderate to severe osteoarthritis of the knee: results of a 24-week, randomized, controlled, phase 1 study. Osteoarthritis Cartilage. 2017 Oct;25(10):1598-1606. doi: 10.1016/j.joca.2017.07.006. Epub 2017 Jul 13. PubMed PMID: 28711582.

 

Products are for research use only. Not for human use.

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