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Wnt-C59 (Synonyms: PORCN Inhibitor II)

Catalog No.GC13658

PORCN inhibitor,highly potent and selective

Products are for research use only. Not for human use. We do not sell to patients.

Wnt-C59 Chemical Structure

Cas No.: 1243243-89-1

Size Price Stock Qty
10mM (in 1mL DMSO)
$123.00
In stock
5mg
$64.00
In stock
10mg
$98.00
In stock
50mg
$437.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Human CC cell lines, CC-LP-1, SNU-1079, WITT-1, SNU-1196, and CC-SW-1

Preparation method

The solubility of this compound in DMSO is > 19 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

100 nM, 10 d

Applications

Inhibition of PORCN with Wnt-C59 leaded to a reduction in cell count in a dose-dependent manner in all 5 cell lines. Treating CC cells with Wnt-C59 resulted in reduction of BrdU uptake and increase of caspase-3/7 activity, indicating reduced proliferation and increased apoptosis of CC cells.

Animal experiment [2]:

Animal models

Female MMTV-WNT1 mice with mammary tumors

Dosage form

Oral administration, 5 mg/kg

Application

Wnt-C59 inhibited the progression of mammary tumors in MMTV-WNT1 transgenic mice and reduced Wnt/β-catenin expression. Furthermore, Wnt-C59 exhibited good bioavailability and no apparent toxicity to mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Boulter L, Guest R V, Kendall T J, et al. WNT signaling drives cholangiocarcinoma growth and can be pharmacologically inhibited[J]. The Journal of clinical investigation, 2015, 125(3): 1269-1285.

[2]. Proffitt K D, Madan B, Ke Z, et al. Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer[J]. Cancer research, 2013, 73(2): 502-507.

Background

Wnt-C59 is a selective inhibitor of Wnt signaling with IC50 value of 74 pM [1].

Wnt signaling pathways are a group of signal transduction pathways made of proteins and play an important role in passing signals from outside of a cell through cell surface receptors to the inside of the cell [1, 2].

Wnt-C59 is a potent Wnt inhibitor and has a different selectivity with the reported Wnt inhibitor crizotinib. When tested with HT1080 and Hela cells, Wnt-C59 showed inhibition on activation of a multimerized TCF-binding site driving luciferase mediated by Wnt3A by completely abrogating Wnt secretion [1]. In 5 human CC cell lines CC-LP-1, SUN-1079, WITT-1, SNU-1196, and CC-SW-1, Wnt-C59 treatment decreased cell viability, reduced cell proliferation and increased cell apoptosis by inhibiting Wnt signaling [2].

In C57/BL6 mice model transplanted with fragments from 2 independent primary MMTV-WNT1 tumors, oral administration of Wnt-C59 (10 mg/kg/d) for 17 days significantly arrested tumor growth and decreased tumor weights after sacrificing mice [1]. When tested with CD1 nude mice model with CC cell lines (CC-LP-1 and CC-SW-1) subcutaneous xenograft into the flanks, administration ofWnt-C59 inhibited cell growth and increased cell apoptosis compared with control group [2].

References:
[1].  Proffitt, K.D., et al., Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer. Cancer Res, 2013. 73(2): p. 502-7.
[2].  Boulter, L., et al., WNT signaling drives cholangiocarcinoma growth and can be pharmacologically inhibited. J Clin Invest, 2015. 125(3): p. 1269-85.

Chemical Properties

Cas No. 1243243-89-1 SDF
Synonyms PORCN Inhibitor II
Chemical Name 2-[4-(2-methylpyridin-4-yl)phenyl]-N-(4-pyridin-3-ylphenyl)acetamide
Canonical SMILES CC1=NC=CC(=C1)C2=CC=C(C=C2)CC(=O)NC3=CC=C(C=C3)C4=CN=CC=C4
Formula C25H21N3O M.Wt 379.45
Solubility ≥ 18.95mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.6354 mL 13.177 mL 26.3539 mL
5 mM 0.5271 mL 2.6354 mL 5.2708 mL
10 mM 0.2635 mL 1.3177 mL 2.6354 mL
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Average Rating: 5 ★★★★★ (Based on Reviews and 37 reference(s) in Google Scholar.)

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