产品名称
4-Hydroxytamoxifen Ready Made Solution, 5 mg/mL in ethanol: isopropanol (95:5)
生物来源
synthetic
质量水平
表单
solution
浓度
5 mg/mL in ethanol: isopropanol (95:5)
运输
dry ice
储存温度
−20°C
SMILES字符串
N(CCOc1ccc(cc1)\C(=C(\CC)/c3ccccc3)\c2ccc(cc2)O)(C)C
InChI
1S/C26H29NO2/c1-4-25(20-8-6-5-7-9-20)26(21-10-14-23(28)15-11-21)22-12-16-24(17-13-22)29-19-18-27(2)3/h5-17,28H,4,18-19H2,1-3H3/b26-25-
InChI key
TXUZVZSFRXZGTL-QPLCGJKRSA-N
相关类别
生化/生理作用
4-羟基他莫昔芬是他莫昔芬的活性代谢产物。
4-羟基他莫昔芬是他莫昔芬的活性代谢产物。4-羟基他莫昔芬在人肝脏中由细胞色素 P450 2D6 形成，是一种强效选择性雌激素受体拮抗剂。4-羟基他莫昔芬用于刺激 LC3 脂化，并以超氧化物依赖的方式形成自噬囊泡。在原代培养的人肝细胞中，他莫昔芬和 4-羟基他莫昔芬显著诱导细胞色素 P450 3A4（一种主要的药物代谢酶）。4-羟基他莫昔芬经历反 (E-Z) 异构化—这一过程发生在所有常见的实验室溶剂中。
4-羟基他莫昔芬的反式 异构体具有抗雌激素活性，而 顺式 4-羟基他莫昔芬是雌激素受体的关键激动剂。4-羟基他莫昔芬通过激活 乳腺癌细胞中p38 通路促进凋亡。
制备说明
4-羟基他莫昔芬为 13 mM 溶液。推荐工作浓度为 10-100μM。因此，4-羟基他莫昔芬制备液应在细胞培养基中以 1:130-1:1,300 稀释。
警示用语：
Danger
危险分类
Aquatic Chronic 3 - Carc. 1B - Eye Irrit. 2 - Flam. Liq. 2 - Repr. 1B
储存分类代码
3 - Flammable liquids
WGK
WGK 3
闪点(°F)
55.4 °F
闪点(°C)
13 °C
法规信息
危险化学品
此项目有
Characterization of tamoxifen and 4-hydroxytamoxifen glucuronidation by human UGT1A4 variants.
Sun D, et al.
Breast Cancer Research, 8(4), R50-R50 (2006)
Activation of the p38 mitogen-activated protein kinase pathway by estrogen or by 4-hydroxytamoxifen is coupled to estrogen receptor-induced apoptosis.
Zhang C C and Shapiro D J
The Journal of Biological Chemistry, 275(1), 479-486 (2000)
Izumi Kaji et al.
JCI insight, 6(16) (2021-07-02)
Functional loss of myosin Vb (MYO5B) induces a variety of deficits in intestinal epithelial cell function and causes a congenital diarrheal disorder, microvillus inclusion disease (MVID). The impact of MYO5B loss on differentiated cell lineage choice has not been investigated.
Jinming Zhao et al.
iScience, 24(12), 103425-103425 (2021-12-09)
We previously showed stabilization of NIK-induced activation of NF-κB non-canonical signaling suppresses MLL-AF9-induced AML. In the current study, we demonstrate that deletion of NF-κB non-canonical RelB prevents the inhibitory effect of NIK stabilization in MLL-AF9 AML. Mechanistically, RelB suppresses its
Kindlin-2 preserves integrity of the articular cartilage to protect against osteoarthritis.
Wu, et al.
Nature aging, 2, 332-347 (2023)
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