1. Stem Cell/Wnt
  2. Wnt

JW74 

Cat. No.: HY-19739 Purity: 99.93%
Handling Instructions

JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling with an IC50 of 420 nM.

For research use only. We do not sell to patients.
JW74 Chemical Structure

JW74 Chemical Structure

CAS No. : 863405-60-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 106 In-stock
5 mg USD 96 In-stock
10 mg USD 144 In-stock
25 mg USD 288 In-stock
50 mg USD 480 In-stock
100 mg USD 840 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.1905 mL 10.9524 mL 21.9048 mL
5 mM 0.4381 mL 2.1905 mL 4.3810 mL
10 mM 0.2190 mL 1.0952 mL 2.1905 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[2]

JW74 is dissolved in DMSO and then diluted in culturing medium before use[2].

The cell lines U2OS, SaOS-2, and KPD are cultured in RPMI-1640. Two to three thousand cells attached overnight in 96-well plates are treated with culturing medium containing 0.1% DMSO (control) or JW74 (10-0.1 μM). Proliferation rates based on cell confluence are determined by live cell imaging. Cellular viability is also determined by MTS assay. Expression of the proliferation marker Ki-67 is performed by staining cells with PE-mouse anti-human Ki-67 and by analyzing the expression by flow cytometry[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

JW74 is prepared in 1% Tween-80[1].

Mice[1]
40 female C.B-Igh-1b/IcrTac-Prkdcscid mice are injected subcutaneously (s.c.) at the right posterior flank with 107 SW480 cells diluted in 100 μL PBS. Injections are initiated when tumor formation is visible in 50 % of the animals (7 days). Mice are randomized and divided into three treatment groups: JW74 150 mg/kg, JW74 300 mg/kg and vehicle control, 1 % Tween 80. Daily intra peritoneal (i.p.) injections (200 μL) with two day injection intermissions after every fifth injection day are performed until the experiment end (29 days). At the termination day, 24 hours after the last injection, blood is collected after cardiac puncture and tumors are dissected and weighed. The compound concentration in tumors and blood are determined using on-line and off-line Solid Phase Extraction-Capillary Liquid Chromatography (SPE-CapLC) instrumentation coupled to a Time of Flight (TOF) mass spectrometer. A Zorbax SB C18 5 μm 150×0.3 mm column is used for separation, and a Knauer K-2600 UV detector is used as a complimentary detector.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

456.52

Formula

C₂₄H₂₀N₆O₂S

CAS No.

863405-60-1

SMILES

CC1=CC=C(C2=NOC(CSC3=NN=C(C4=CC=NC=C4)N3C5=CC=C(OC)C=C5)=N2)C=C1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
JW74
Cat. No.:
HY-19739
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