Oxyphenisatine (Oxyphenisatin)
(Synonyms: 酚汀; Oxyphenisatin) 目录号 : GC34107Oxyphenisatine (Oxyphenisatin) (Oxyphenisatin) 是一种泻药。 Oxyphenisatin acetate 是 oxyphenisatin 的前体药物,具有抗癌活性。
Cas No.:125-13-3
Sample solution is provided at 25 µL, 10mM.
Oxyphenisatine (Oxyphenisatin) is a laxative. Oxyphenisatin acetate is the pro-drug of oxyphenisatin with anticancer activity.
Oxyphenisatin has been shown to have antiproliferative activity. Oxyphenisatin acetate (OXY, NSC 59687) is the pro-drug of oxyphenisatin. OXY inhibits the growth of the breast cancer cell lines MCF7, T47D, HS578T, and MDA-MB-468 (IC50=0.8, 0.6, 2.1, 1.8 μM). This effect is associated with selective inhibition of translation accompanied by rapid phosphorylation of the nutrient sensing eIF2α kinases, GCN2 and PERK[1].
Toxicity studies demonstrate that mice tolerate IP administration of OXY at 300 mg/kg once daily or 200 mg/kg twice daily. Administration of OXY at 300 mg/kg IP once daily for 10 days results in significantly smaller tumors from day 33 to day 52[1].
[1]. Morrison BL, et al. Oxyphenisatin acetate (NSC 59687) triggers a cell starvation response leading to autophagy, mitochondrial dysfunction, and autocrine TNFα-mediated apoptosis. Cancer Med. 2013 Oct;2(5):687-700.
Animal experiment: | Mice: When tumors reaches 120 mg, mice are randomized into treatment groups and therapy is initiated. Asimple toxicity assessment to determine tolerability to OXY is conducted by administering single intraperitoneal (IP) doses of compound at 100, 200, and 400 mg/kg. The mice were observed for adverse effects for 14 days postdose[1]. |
References: [1]. Morrison BL, et al. Oxyphenisatin acetate (NSC 59687) triggers a cell starvation response leading to autophagy, mitochondrial dysfunction, and autocrine TNFα-mediated apoptosis. Cancer Med. 2013 Oct;2(5):687-700. |
Cas No. | 125-13-3 | SDF | |
别名 | 酚汀; Oxyphenisatin | ||
Canonical SMILES | O=C1NC2=C(C=CC=C2)C1(C3=CC=C(O)C=C3)C4=CC=C(O)C=C4 | ||
分子式 | C20H15NO3 | 分子量 | 317.34 |
溶解度 | DMSO : ≥ 28 mg/mL (88.23 mM) | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.1512 mL | 15.756 mL | 31.5119 mL |
5 mM | 0.6302 mL | 3.1512 mL | 6.3024 mL |
10 mM | 0.3151 mL | 1.5756 mL | 3.1512 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。
Quality Control & SDS
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- Purity: >98.00%
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