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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $35 | In Stock | |
5 mg | $56 | In Stock | |
10 mg | $73 | In Stock | |
25 mg | $163 | In Stock | |
50 mg | $247 | In Stock | |
100 mg | $347 | In Stock | |
1 mL x 10 mM (in DMSO) | $62 | In Stock |
Description | JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling (IC50: 420 nM). |
In vitro | Ki-67 expression is reduced from 97.5% in DMSO-treated cells to 86.7% in JW74-treated cells. Relative to DMSO-treated cells, the cellular viability of U2OS cells treated for 72 h treatment with 10 μM JW74 is reduced to 80%. The effect of tankyrase inhibition on cellular viability is tested by performing an MTS assay. Flow cytometry is also performed to determine the expression marker Ki-67 in U2OS following 48 h treatment with DMSO or 10 uM JW74 [2]. JW74 displays a reduction of canonical Wnt signaling in the ST-Luc assay (IC50: 790 nM) [1]. |
In vivo | The in vivo efficacy of JW74 is tested using SW480 cell xenografts. A relatively high dose of JW74 (150 or 300 mg/kg) is used because of a rapid compound degradation in the organism as indicated in the human liver microsome analysis (t1/2=2.5 minutes) and in pharmacokinetic analyses (after peroral injections: t1/2=30 minutes and intravenous injections: t1/2=15 minutes). JW74 concentration in tumors is in the range 4.2 to 72.1 μmol/kg for JW74 150 mg/kg, 1.9 to 11.1 μmol/kg for JW74 300 mg/kg, and 2.8 μM in plasma for both doses [1]. |
Molecular Weight | 456.52 |
Formula | C24H20N6O2S |
Cas No. | 863405-60-1 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (98.57 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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