2. Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. EGFR Apoptosis
  4. HER2-IN-22

HER2-IN-22 是一种强效且具有选择性的 HER2 抑制剂，其 IC50 值为 215 μM。HER2-IN-22 对多种肿瘤细胞具有杀伤活性，并能诱导细胞凋亡 (apoptosis)。HER2-IN-22 显著抑制小鼠体内肿瘤增长。HER2-IN-22 可用于 HER2+ 乳腺癌等肿瘤研究。

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HER2-IN-22 Chemical Structure

HER2-IN-22 Chemical Structure

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HER2-IN-22 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

查看所有亚型
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HER2-IN-22 is a potent and selective HER2 inhibitor with an IC50 of 215 μM. HER2-IN-22 possesses killing activity against various tumor cells and can induce cell apoptosis. HER2-IN-22 significantly inhibits tumor growth. HER2-IN-22 can be used in the study for tumors such as HER2+ breast cancer[1].

IC50 & Target[1]

HER2

215 μM (IC50)

体外研究
(In Vitro)

HER2-IN-22 (compound 3f) 在 NCI 60 细胞系中对白血病、中枢神经系统和乳腺癌细胞系的平均 GI50 值分别为 1.9、2.5 和 2.3 μM[1]。
HER2-IN-22 (10 μM, 30 min) 对 HER2 的抑制作用达到 88%[1]。
HER2-IN-22 (0.05-250 μM, 30 min) 对 HER2 激酶的 IC50 值为 215 μM[1]。
HER2-IN-22 (0-50 μM, 72 h) 对 BT474、BT549 和 ZR-75-30 的抗增殖活性较高，其 IC50 分别为 323.3、282.6 和 271.7 nM[1]。
HER2-IN-22 (0.5-10 μM, 72 h) 在 BT474 细胞中诱导了最高的坏死水平，在 10μM 时达到 10.5%。[1]。

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

HER2-IN-22 相关抗体:

Apoptosis Analysis[1]

Cell Line: BT474
Concentration: 0.5 μM, 1 μM, 5 μM, 10 μM
Incubation Time: 72 h
Result: Induced a negligible level of early (4.7%) and late apoptosis (3%) at 5 μM.
Induced the highest necrotic level at 10 μM of 10.5 %.
体内研究
(In Vivo)

HER2-IN-22 (compound 3f) (10 mg/kg; i.p.; single dose) 在小鼠体内乳腺癌模型中表现出了抗肿瘤活性[1]。

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

Animal Model: Xenograft mouse model by 6-week-old female nude mice injected with 100 μL of ZR-75-30-luciferase 2×106 cells[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; after 1 and 7 weeks using the In Vivo Imaging System; tumor volume was measured twice a week for 7 weeks; histopathological analysis by the end of week 7
Result: Had lower bioluminescence intensities.
Showed a significant inhibition in tumor size by 19.45%.
Reduced the tumor weight (p = 0.041) at the end of the experiment.
分子量

576.24

Formula

C26H16Br2N4O2
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

HER2-IN-22 相关分类

  • 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.

Keywords:

HER2-IN-22EGFRApoptosisEpidermal growth factor receptorErbB-1HER1PyrazolopyridinesAntitumorDockingMolecular dynamicsBreast cancerBT474Inhibitorinhibitorinhibit

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