Wnt-C59
(Synonyms: PORCN酶活性和WNT抑制剂(WNT-C59),C59) 目录号 : GC13658
A potent Porcupine inhibitor
Cas No.:1243243-89-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Human CC cell lines, CC-LP-1, SNU-1079, WITT-1, SNU-1196, and CC-SW-1 |
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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. |
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Reacting condition |
100 nM, 10 d |
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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]: | |
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Animal models |
Female MMTV-WNT1 mice with mammary tumors |
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Dosage form |
Oral administration, 5 mg/kg |
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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. |
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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. |
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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. | |
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.
| Cas No. | 1243243-89-1 | SDF | |
| 别名 | PORCN酶活性和WNT抑制剂(WNT-C59),C59 | ||
| 化学名 | 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 | ||
| 分子式 | C25H21N3O | 分子量 | 379.45 |
| 溶解度 | ≥ 18.95mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。