JW74

Name: JW74
Brand: MedChemExpress
SKU: HY-19739
Rating: 5.0 (4 reviews)

Cat. No.: HY-19739 Purity: 99.34%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 863405-60-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 77	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 77	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
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Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE JW74

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Description

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

IC₅₀ & Target

IC50: 420 nM (Wnt)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.548 μM Compound: 3, JW74	Inhibition of mouse Wnt3A signaling in human HEK293 cells after 1 day by super top flash luciferase reporter gene assay Inhibition of mouse Wnt3A signaling in human HEK293 cells after 1 day by super top flash luciferase reporter gene assay	[PMID: 22260203]
HEK293	IC₅₀	1.01 μM Compound: 1, JW74	Inhibition of TNKS1/2 in HEK293 cells assessed as inhibition of Wnt/beta-casein pathway after 24 hrs by luciferase reporter gene assay Inhibition of TNKS1/2 in HEK293 cells assessed as inhibition of Wnt/beta-casein pathway after 24 hrs by luciferase reporter gene assay	[PMID: 23473363]
SW480	EC₅₀	0.566 μM Compound: 3, JW74	Stabilization of Axin2 in human SW480 cells after 24 hrs by sandwich ELISA Stabilization of Axin2 in human SW480 cells after 24 hrs by sandwich ELISA	[PMID: 22260203]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 (t_1/2=2.5 minutes) and in pharmacokinetic analyses (after per oral injections: t_1/2=30 minutes and intravenous injections: t_1/2=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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

456.52

Formula

C₂₄H₂₀N₆O₂S

CAS No.

863405-60-1

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (109.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.75 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.34%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (257 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Waaler J, et al. Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth. Cancer Res. 2011 Jan 1;71(1):197-205. [Content Brief]

[2]. Stratford EW, et al. The tankyrase-specific inhibitor JW74 affects cell cycle progression and induces apoptosis and differentiation in osteosarcoma cell lines. Cancer Med. 2014 Feb;3(1):36-46. [Content Brief]

Cell Assay ^[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]	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	[1]. Waaler J, et al. Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth. Cancer Res. 2011 Jan 1;71(1):197-205. [Content Brief] [2]. Stratford EW, et al. The tankyrase-specific inhibitor JW74 affects cell cycle progression and induces apoptosis and differentiation in osteosarcoma cell lines. Cancer Med. 2014 Feb;3(1):36-46. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1905 mL	10.9524 mL	21.9048 mL	54.7621 mL
	5 mM	0.4381 mL	2.1905 mL	4.3810 mL	10.9524 mL
	10 mM	0.2190 mL	1.0952 mL	2.1905 mL	5.4762 mL
	15 mM	0.1460 mL	0.7302 mL	1.4603 mL	3.6508 mL
	20 mM	0.1095 mL	0.5476 mL	1.0952 mL	2.7381 mL
	25 mM	0.0876 mL	0.4381 mL	0.8762 mL	2.1905 mL
	30 mM	0.0730 mL	0.3651 mL	0.7302 mL	1.8254 mL
	40 mM	0.0548 mL	0.2738 mL	0.5476 mL	1.3691 mL
	50 mM	0.0438 mL	0.2190 mL	0.4381 mL	1.0952 mL
	60 mM	0.0365 mL	0.1825 mL	0.3651 mL	0.9127 mL
	80 mM	0.0274 mL	0.1369 mL	0.2738 mL	0.6845 mL
	100 mM	0.0219 mL	0.1095 mL	0.2190 mL	0.5476 mL

JW74 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JW74863405-60-1JW 74JW-74WntInhibitorinhibitorinhibit

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JW74

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4 Publications Citing Use of MCE JW74

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Complete Stock Solution Preparation Table

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