Endoxifen hydrochloride
(Synonyms: 因多昔芬盐酸盐) 目录号 : GC35990
Endoxifen hydrochloride 是 Tamoxifen 的活性代谢物，是有效的雌激素受体 (estrogen receptor) 拮抗剂。
Cas No.:1197194-41-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Endoxifen hydrochloride, the active metabolite of Tamoxifen, is a potent antiestrogen that targets estrogen receptor. Estrogen receptor[1]
Endoxifen blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. These studies reveal that Endoxifen concentrations between 10 and 1000 nM enhance ERα protein degradation. Lower concentrations of Endoxifen (≤1 nM) do not affect ERα protein levels[1].
GLAST::Cre(ERT);ROSA26loxP/loxP mice are injected intraventricularly with 5 μL 5 mM Endoxifen, and mice injected with 4 μL Adeno-Cre virus [109 plaque-forming units (pfu)] serve as positive control. At 7-10 days after ICV injection, mice are sacrificed and the SVZ dissected to isolate and derive stem and progenitor cells. These stem/progenitor cells are then cultured in permissive medium to form neurospheres and assayed for recombination. In our unpassaged preparations is found derived from Endoxifen-injected GLAST::CreERT2;ROSA26loxP/loxP mice that 1.9% of neurospheres show recombination, compared to a higher rate of 4.3% of neurospheres in Adeno-Cre-recombined ROSA26loxP/loxP mice[2].
[1]. Wu X, et al. The tamoxifen metabolite, Endoxifen, is a potent antiestrogen that targets estrogen receptor alpha fordegradation in breast cancer cells. Cancer Res. 2009 Mar 1;69(5):1722-7. [2]. Benedykcinska A, et al.Generation of brain tumours in mice by Cre-mediated recombination of neural progenitors in situ with the tamoxifen metabolite Endoxifen. Dis Model Mech. 2016 Feb;9(2):211-20.
| Cas No. | 1197194-41-4 | SDF | |
| 别名 | 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 | ||
| 分子式 | C25H28ClNO2 | 分子量 | 409.95 |
| 溶解度 | DMSO: ≥ 35 mg/mL (85.38 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 | |||
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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 |
| 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。
The effects of a novel hormonal breast cancer therapy, endoxifen, on the mouse skeleton
PLoS One 2014 May 22;9(5):e98219.PMID:24853369DOI:10.1371/journal.pone.0098219.
Endoxifen has recently been identified as the predominant active metabolite of tamoxifen and is currently being developed as a novel hormonal therapy for the treatment of endocrine sensitive breast cancer. Based on past studies in breast cancer cells and model systems, endoxifen classically functions as an anti-estrogenic compound. Since estrogen and estrogen receptors play critical roles in mediating bone homeostasis, and endoxifen is currently being implemented as a novel breast cancer therapy, we sought to comprehensively characterize the in vivo effects of endoxifen on the mouse skeleton. Two month old ovariectomized C57BL/6 mice were treated with vehicle or 50 mg/kg/day Endoxifen hydrochloride via oral gavage for 45 days. Animals were analyzed by dual-energy x-ray absorptiometry, peripheral quantitative computed tomography, micro-computed tomography and histomorphometry. Serum from control and endoxifen treated mice was evaluated for bone resorption and bone formation markers. Gene expression changes were monitored in osteoblasts, osteoclasts and the cortical shells of long bones from endoxifen treated mice and in a human fetal osteoblast cell line. Endoxifen treatment led to significantly higher bone mineral density and bone mineral content throughout the skeleton relative to control animals. Endoxifen treatment also resulted in increased numbers of osteoblasts and osteoclasts per tissue area, which was corroborated by increased serum levels of bone formation and resorption markers. Finally, endoxifen induced the expression of osteoblast, osteoclast and osteocyte marker genes. These studies are the first to examine the in vivo and in vitro impacts of endoxifen on bone and our results demonstrate that endoxifen increases cancellous as well as cortical bone mass in ovariectomized mice, effects that may have implications for postmenopausal breast cancer patients.