Endoxifen Z-isomer hydrochloride
(Synonyms: Z-因多昔芬盐酸盐) 目录号 : GC35991Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
Cas No.:1032008-74-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. [1] Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. [2] In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation. [3] Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen. [4] Endoxifen inhibits the hERG current by preferentially interacting with the activated states of cloned hERG potassium channels with IC50 of 1.6 μM. [5]
In vivo, Endoxifen (8 mg/kg, ) inhibits growth of MCF-7 human mammary tumor xenografts in mice, showing more potency than Tamoxifen. [3]
[1] Lim YC, et al. Cancer Chemother Pharmacol. 2005, 55(5), 471-478. [2] Wu X, et al. Cancer Res. 2009, 69(5), 1722-1727. [3] Ahmad A, et al. Breast Cancer Res Treat. 2010, 122(2), 579-584.
Cas No. | 1032008-74-4 | SDF | |
别名 | Z-因多昔芬盐酸盐 | ||
Canonical SMILES | OC1=CC=C(/C(C2=CC=C(OCCNC)C=C2)=C(C3=CC=CC=C3)\CC)C=C1.[H]Cl.[Z] | ||
分子式 | C25H28ClNO2 | 分子量 | 409.95 |
溶解度 | DMSO: 12.5 mg/mL (30.49 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.4393 mL | 12.1966 mL | 24.3932 mL |
5 mM | 0.4879 mL | 2.4393 mL | 4.8786 mL |
10 mM | 0.2439 mL | 1.2197 mL | 2.4393 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 | |||
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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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