Acolbifene
(Synonyms: EM-652; SCH 57068) 目录号 : GC18362A selective estrogen receptor modulator
Cas No.:182167-02-8
Sample solution is provided at 25 µL, 10mM.
Acolbifene is a selective estrogen receptor modulator (SERM). It inhibits transcriptional activity of estrogen receptor α (ERα) and ERβ induced by estradiol . It binds to ERs in cytosol from human breast cancer and non-cancerous uterine cells (Kis = 0.047 and 0.042 nM, respectively) and to ERs in cytosol from rat uterine cells (IC50 = 0.44 nM) but not to progesterone or androgen receptors in cytosol from rat uterine and ventral prostate cells (IC50s = 22,500 and >10,000 nM, respectively). Acolbifene inhibits E2-stimulated proliferation of T47D, ZR-75-1, and MCF-7 breast cancer cells (IC50s = 0.146, 0.75, and 0.321 nM, respectively) but not basal proliferation. Acolbifene (50 μg per day) inhibits tumor growth stimulated by estrone in a ZR-75-1 human breast cancer xenograft model in ovariectomized mice. It also inhibits E1-stimulated endometrial epithelium thickening in vivo in ovariectomized mice when administered at a dose of 50 μg per day.
References:
[1].Labrie, F., Labrie, C., Bélanger, A., et al. EM-652 (SCH 57068), a third generation SERM acting as pure antiestrogen in the mammary gland and endometrium J. Steroid Biochem. Mol. Biol. 69(1-6), 51-84 (1999).
[2]. Martel, C., Provencher, L., Li, X., et al. Binding characteristics of novel nonsteroidal antiestrogens to the rat uterine estrogen receptors J. Steroid Biochem. Mol. Biol. 64(3-4), 199-205 (1998).
[3]. Gutman, M., Couillard, S., Roy, J., et al. Comparison of the effects of EM-652 (SCH57068), tamoxifen, toremifene, droloxifene, idoxifene, GW-5638 and raloxifene on the growth of human ZR-75-1 breast tumors in nude mice Int. J. Cancer 99(2), 273-278 (2002).
Cas No. | 182167-02-8 | SDF | |
别名 | EM-652; SCH 57068 | ||
化学名 | (2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-2H-1-benzopyran-7-ol | ||
Canonical SMILES | OC1=CC=C(C(C)=C(C2=CC=C(O)C=C2)[C@H](C3=CC=C(OCCN4CCCCC4)C=C3)O5)C5=C1 | ||
分子式 | C29H31NO4 | 分子量 | 457.6 |
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 | 2.1853 mL | 10.9266 mL | 21.8531 mL |
5 mM | 0.4371 mL | 2.1853 mL | 4.3706 mL |
10 mM | 0.2185 mL | 1.0927 mL | 2.1853 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: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet