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CAS No.: 1467093-03-3

Adavivint Catalog No. CSN22337

Synonyms: SM04690;Lorecivivint

Adavivint 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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技术信息

生物活性

描述The Wnt pathway plays an important role in cell differentiation, organogenesis, morphogenesis, and tissue remodeling. Adavivint is a small-molecule Wnt pathway inhibitor with an EC50 value of 19.5nM for the TCF/LEF reporter but had no effect on the SV40 luciferase reporter. Treatment of bone-marrow-derived human mesenchymal stem cells (hMSCs; CD29+, CD44+, CD166+, CD105+, CD45−) with 30nM adavivint resulted in a concentration-dependent decrease in the expression of Wnt pathway genes (ASCL1, LEF1, TCF7L2, TCF7, C-MYC, and AXIN2). Adavivint also dose-dependently promoted the aggregation of hMSCs with an EC50 value of 10nM. Compared to DMSO-treated controls, hMSCs treated with adavivint (30nM) for 3 days showed significantly increased expression of Sox9. Adavivint treatment also downregulated the genes associated with tendon or ligament differentiation (COL1A1) and osteoblast differentiation (osteocalcin, alkaline phosphatase, BMP4, RUNX2) in hMSCs. Treatment of adavivint (30nM) for 21 days induced chondrocyte differentiation in mouse chondrogenic ATDC5 cells. Primary mouse embryo calvarial cells exposed to 100 nM of adavivint for 21 days showed increased number and size of Alcian Blue stained chondrocytes compared with DMSO-treated controls. A single IA injection of adavivint (0.3 μg) promoted cartilage growth, improved joint health, decreased cartilage breakdown, and inhibited the Wnt pathway in a rat model of knee osteoarthritis^[1].
参考文献

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 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

技术信息

CAS号

1467093-03-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H24FN7O

运输

蓝冰

分子量

505.55

别名

SM04690;Lorecivivint

溶解度

DMSO	30.0 mg/mL (59.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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