WYC-209
(Synonyms: 4,5-二(羟甲基)-2-苯基-1H-咪唑) 目录号 : GC34862
WYC-209是一种合成类视黄醇，能抑制恶性小鼠黑色素瘤肿瘤再生细胞(TRC)的增殖，IC50值为0.19μM。WYC-209主要细胞靶点是维甲酸受体(RARs)。
Cas No.:2131803-90-0
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
WYC-209 is a synthetic retinoid, which inhibits proliferation of malignant murine melanoma tumor-repopulating cells (TRCs) with an IC50 of 0.19 μM. The primary cellular target of WYC-209 is retinoic acid receptors (RARs)[1]. Retinoic acid receptors[1]
[1]. Chen J, et al. Inhibition of cancer stem cell like cells by a synthetic retinoid. Nat Commun. 2018 Apr 11;9(1):1406.
| Cas No. | 2131803-90-0 | SDF | |
| 别名 | 4,5-二(羟甲基)-2-苯基-1H-咪唑 | ||
| Canonical SMILES | O=C(C1=CN=C(C#CC2=CC=C3C(C(C)(C)CCS3=O)=C2)N=C1)OCC | ||
| 分子式 | C20H20N2O3S | 分子量 | 368.45 |
| 溶解度 | DMSO : 83.33 mg/mL (226.16 mM);Water : < 0.1 mg/mL (insoluble) | 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 | 2.7141 mL | 13.5704 mL | 27.1407 mL |
| 5 mM | 0.5428 mL | 2.7141 mL | 5.4281 mL |
| 10 mM | 0.2714 mL | 1.357 mL | 2.7141 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。
Inhibition of cancer stem cell like cells by a synthetic retinoid
Nat Commun 2018 Apr 11;9(1):1406.PMID:29643385DOI:PMC5895803
Developing novel drugs that can abrogate the growth and metastasis of malignant tumors is a major challenge for cancer researchers. Here we describe a novel synthetic retinoid, namely WYC-209, which inhibits proliferation of malignant murine melanoma tumor-repopulating cells (TRCs), known to resist conventional drug treatment, with an IC50 of 0.19 μM in a dose-dependent manner. WYC-209 also inhibits proliferation of TRCs of human melanoma, lung cancer, ovarian cancer, and breast cancer in culture. Interestingly, the treated TRCs fail to resume growth even after the drug washout. Importantly, the molecule abrogates 87.5% of lung metastases of melanoma TRCs in immune-competent wild-type C57BL/6 mice at 0.22 mg kg-1 without showing apparent toxicity. Pretreating the melanoma TRCs with retinoic acid receptor (RAR) antagonists or with RAR siRNAs blocks or reduces the inhibitory effect of the molecule, suggesting that the target of the molecule is RAR. WYC-209 induces TRC apoptosis and pretreating the TRCs with caspase 3 inhibitor or depleting caspase 3 with siRNAs substantially rescues growth of TRCs from WYC-209 inhibition, suggesting that WYC-209 induces TRCs apoptosis primarily via the caspase 3 pathway. Our findings demonstrate the promise of the new retinoid WYC-209 in treating malignant melanoma tumors with high efficacy and little toxicity.