20-HEDE (WIT 002)
(Synonyms: WIT 002) 目录号 : GC33412
20-HEDE (WIT 002) (WIT 002) 是 20-羟基二十碳四烯酸 (20-HETE) 的拮抗剂。
Cas No.:240427-90-1
Sample solution is provided at 25 µL, 10mM.
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WIT 002 is an antagonist of 20-hydroxyeicosatetraenoic acid (20-HETE).
ω-hydroxylation activity toward arachidonic acid is high in A549 cells, thus, A549 cells are treated with HET0016 or WIT 002 in the invasion assays, and both of them significantly decrease invasion[2]. WIT 002 inhibits proliferation of 786-O and 769-P renal adenocarcinoma cells, but HET0016 and WIT 002 fail to inhibit proliferation of normal renal epithelial cells RPTC[2][3].
The effect of the 20-HETE antagonist, WIT 002 on the growth of 786-O clear cell renal carcinoma is assessed in ectopic mouse model of renal tumor. The growth of tumors is significantly suppressed by WIT 002 administered daily to athymic nude mice implanted subcutaneously with cells 786-O. Tumor growth is inhibited by 84%±128%. It is of note that in these experiments WIT 002 treatment start only after the tumor is seeded for 7-14 days and is relatively large 0.1 cm. Thus, WIT 002 is effective at arresting the growth of a fairly advanced tumor[3].
[1]. Ming Yua . et al. Effects of a 20-HETE antagonist and agonists on cerebral vascular tone. Eur J Pharmacol. 2004 Feb 23;486(3):297-306. [2]. Wei Yu, et al. Cytochrome P450 ω-hydroxylase promotes angiogenesis and metastasis by upregulation of VEGF and MMP-9 in non-small cell lung cancer. Cancer Chemother Pharmacol. 2011 Sep; 68(3): 619-29. [3]. Anna Alexanian, et al. Down-regulation of 20-HETE Synthesis and Signaling Inhibits Renal Adenocarcinoma Cell Proliferation and Tumor Growth. Anticancer Res. 2009 October ; 29(10): 3819-3824.
Cell experiment: | Human NSCLC cell lines (e.g A549) are seeded onto the upper well of the chamber. Subsequently, serum-free medium with HET0016 (10 μM), WIT002 (10 μM), WIT003 (0.01, 0.1, 1 μM), or ethanol as a control is added to the upper chamber, while the lower well is filled to the top (500 μL) with RPMI-1640 containing 5% fetal calf serum (FCS) as a chemoattractant. Cells are allowed to migrate for 5 h. Cells that have invaded to the bottom surface of the filter are counted with an ocular micrometer in a blinded manner, counting a minimum of 10 high-powered fields (HPF) [2]. Human renal cell adenocarcinoma lines (RPTC) 786-O or 769-P cells are plated and next day (0 hrs) transferred to serum-free medium containing either EGF or ET-1. Cells are exposed either to 10 μM WIT002 or vehicle. Cell counting is performed at the day of transfer to serum free medium (0 hrs) and 24, 48 and 72 hrs thereafter. Medium is changed to fresh containing mitogens and drugs every 24 hrs. Data presented are characteristic experiment from at least two separate experiments, each performed in triplicate[3]. |
Animal experiment: | Mice[3]Experiments are carried out on 6-week immunodefficient athymic nude mice weighing 20-26 g. Animals are acclimated for 1 week prior to injection with renal cell carcinoma. Immediately before each implantation, the cells are trypsinized, counted and resuspended in 10% serum containing RPMI media. The concentration of cells is adjusted to 40 millions/mL and 4 million cells/animal are injected subcutaneously. The cells are allowed to grow for 7-15 days until the size of the tumors reach approximately 0.1 cm3. The mice then receive daily subcutaneous injection (s.c.) injections of WIT 002 (10 mg/kg/day in 200 μL) in an isotonic NaPO4 buffer (pH 9.0) or vehicle (0.1 M NaPO4 solution pH 9.0). The diameter of the tumor is measured on every 3-4 days for 2 weeks using precision calibers. At the end of the experiment the mice are euthanized with CO2 and the tumors were excised to confirm the diameter measurements[3]. |
References: [1]. Ming Yua . et al. Effects of a 20-HETE antagonist and agonists on cerebral vascular tone. Eur J Pharmacol. 2004 Feb 23;486(3):297-306. | |
| Cas No. | 240427-90-1 | SDF | |
| 别名 | WIT 002 | ||
| Canonical SMILES | O=C(O)CCCC/C=C\CCCCCCC/C=C\CCCCO | ||
| 分子式 | C20H36O3 | 分子量 | 324.5 |
| 溶解度 | Soluble 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 | 3.0817 mL | 15.4083 mL | 30.8166 mL |
| 5 mM | 0.6163 mL | 3.0817 mL | 6.1633 mL |
| 10 mM | 0.3082 mL | 1.5408 mL | 3.0817 mL |
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| 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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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。
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Quality Control & SDS
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- Purity: >98.00%
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