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Oxyphenisatine (Oxyphenisatin) Sale

(Synonyms: 酚汀; Oxyphenisatin) 目录号 : GC34107

Oxyphenisatine (Oxyphenisatin) (Oxyphenisatin) 是一种泻药。 Oxyphenisatin acetate 是 oxyphenisatin 的前体药物,具有抗癌活性。

Oxyphenisatine (Oxyphenisatin) Chemical Structure

Cas No.:125-13-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥491.00
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100mg
¥446.00
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Sample solution is provided at 25 µL, 10mM.

Description

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.

实验参考方法

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.

化学性质

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。
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。

溶解性数据

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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
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