1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. Aromatase-IN-8

Aromatase-IN-8 是一种选择性的 aromatase 抑制剂,其对 aromatase 活性的半数抑制浓度 (IC50) 为 0.05 µM。Aromatase-IN-8 对雌激素受体阳性乳腺癌细胞系具有选择性抗增殖作用,同时对非肿瘤细胞无毒性。Aromatase-IN-8 可抑制雌激素活性、提高睾酮水平,并下调雌激素受体的表达与磷酸化。Aromatase-IN-8 可用于三阴乳腺癌研究。

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Aromatase-IN-8

Aromatase-IN-8 Chemical Structure

CAS No. : 1244904-19-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Aromatase-IN-8 is a selective Aromatase inhibitor against an IC50 of 0.05 µM. Aromatase-IN-8 exhibits selective antiproliferative effects against estrogen receptor-positive breast cancer cell lines, while showing no toxicity toward non-tumoral cells. Aromatase-IN-8 suppresses estrogen active, increases testosterone levels, and downregulates estrogen receptor expression and phosphorylation. Aromatase-IN-8 can be used for triple negative breast cancer research[1].

IC50 & Target[1]

Aromatase

0.05 μM (IC50)

体外研究
(In Vitro)

Aromatase-IN-8 (compound 17) (72 小时) 在 ER 阳性乳腺癌细胞系 (T47D 和 MCF-7 细胞) 及三阴性乳腺癌细胞系 (MDA-MB-231 细胞) 中表现出显著的抗癌效果,其 IC50 值分别为 42.90 µM、79.43 µM 和 > 100 µM [1]
Aromatase-IN-8 (6.25-100 µM, 24 及 72 小时) 在 MCF-7 细胞和 MDA-MB-231 细胞中降低细胞活力的效应与剂量增加呈正相关[1]
Aromatase-IN-8 (0-50 μM, 24 小时) 可降低 MCF-7 细胞中的 ERαERβ 蛋白水平[1]
Aromatase-IN-8 (6.25-50 μM, 8小时) 在 MCF-7 细胞中能降低 17β-雌二醇 和雌酮水平,对雌激素合成具有轻微的抑制效果,并在浓度高于 12.5 µM 时导致睾酮更明显的积累[1]
Aromatase-IN-8 可下调脂肪酸降解,上调泛酸与辅酶 A 的生物合成,促进缬氨酸和鞘氨醇的积累,并在 MCF-7 细胞中于较高剂量下表现出强效抗癌作用[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 12.5, 25 and 50 μM
Incubation Time: 24 h
Result: Reduced the expression of both non-phosphorylated and phosphorylated Erα and Erβin a dose-dependent manner.
分子量

346.88

Formula

C17H19ClN4S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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产品名称:
Aromatase-IN-8
目录号:
HY-180535
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