1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage Epigenetics
  2. EGFR PARP
  3. HER2-IN-23

HER2-IN-23 是一种选择性 HER2 抑制剂。HER2-IN-23 降低的是总 HER2 表达,而非磷酸化 HER2 (p-HER2) 的表达。HER2-IN-23 可降低细胞周期蛋白 D1 水平并刺激 PARP 裂解。HER2-IN-23 可用于 HER2 阳性乳腺癌的研究。

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HER2-IN-23

HER2-IN-23 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HER2-IN-23 is a selective HER2 inhibitor. HER2-IN-23 reduces in total HER2 expression rather than in phosphorylated HER2 (p-HER2). HER2-IN-23 reduces cyclin D1 level and stimulates PARP cleavage. HER2-IN-23 can be used for the study of HER2-positive breast cancer[1].

体外研究
(In Vitro)

HER2-IN-23 (Compound 4o) (0.4-25 μM,72 小时) 对 HER2 阳性细胞 (如 BT474 (IC50 = 10.5 μM)、A431 (IC50 = 9.9 μM) 和 HCC1954 (IC50 = 8.5 μM)) 表现出中等的抗增殖活性,但对 HER2 阴性细胞 (如 MDA-MB-231 (IC50 = 19.7 μM) 和 MCF7 (IC50 = 12.8 μM)) 的活性较低[1]
HER2-IN-23 (1 μM) 在 1 μM 浓度下可抑制 HER2 激酶 84%,而对其他激酶 (如 EGFR、HER4、IGF1R 等) 的抑制作用较弱或无抑制作用[1]
HER2-IN-23 (10 μM, 24 h) 显著降低了 A431 细胞中总 HER2 的表达,但磷酸化 HER2 (p-HER2) 没有显著变化;同时,细胞周期蛋白 D1 的表达几乎完全受到抑制,并且观察到 PARP 裂解增加[1]

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

Western Blot Analysis[1]

Cell Line: A431 cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Significantly reduced total HER2 expression in A431 cells, but phosphorylated HER2 (p-HER2) showed no significant change; simultaneously, cyclin D1 expression was almost completely inhibited, and an increase in PARP cleavage was observed.
分子量

398.81

Formula

C22H16ClFO4

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
  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
HER2-IN-23
目录号:
HY-178116
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