Size | Price | Stock |
---|---|---|
5mg | $70 | In-stock |
10mg | $90 | In-stock |
25mg | $200 | In-stock |
50mg | $300 | In-stock |
100mg | $420 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
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Cat. No. : | HY-19739 |
M.Wt: | 456.52 |
Formula: | C24H20N6O2S |
Purity: | >98 % |
Solubility: | DMSO : ≥ 50 mg/mL (109.52 mM) |
JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling with an IC50 of 420 nM. IC50 & Target: IC50: 420 nM (Wnt)[1] In Vitro: JW74 shows a reduction of canonical Wnt signaling in the ST-Luc assay with an IC50 of 790 nM[1]. The effect of tankyrase inhibition on cellular viability is tested by performing an MTS assay. The cellular viability of U2OS cells treated for 72 h treatment with 10 μM JW74 is reduced to 80%, relative to DMSO-treated cells. Flow cytometry is also performed to determine the expression marker Ki-67 in U2OS following 48 h treatment with DMSO or 10 uM JW74. Ki-67 expression is reduced from 97.5% in DMSO-treated cells to 86.7% in JW74-treated cells[2]. 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 per oral injections: t1/2=30 minutes and intravenous injections: t1/2=15 minutes). The presence of JW74 in tumors and plasma is identified by mass spectrometry. 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].
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