1. Protein Tyrosine Kinase/RTK Apoptosis Membrane Transporter/Ion Channel Neuronal Signaling
  2. VEGFR Caspase Calcium Channel
  3. COX-2-IN-55

COX-2-IN-55 (compound 1) 是一种口服有效的 Celecoxib (HY-14398) 类似物,具有广谱的抗癌活性和较弱的 COX-2 抑制作用。COX-2-IN-55 可特异性抑制 SERCA2,增加 caspase-3 裂解和 DR5 水平,从而激活 GRP78,抑制三阴性乳腺癌 (TNBC) 发展。COX-2-IN-55 还可以下调血管生成标志物 VEGF-αIL-8 的水平,抑制微血管的生成。

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COX-2-IN-55 Chemical Structure

COX-2-IN-55 Chemical Structure

CAS No. : 2649115-80-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

COX-2-IN-55 (compound 1) is an orally active, Celecoxib (HY-14398)-based analog with broad-spectrum anticancer activity and weak COX-2 inhibition. COX-2-IN-55 specifically inhibits SERCA2, increases caspase-3 cleavage and DR5 levels, thereby activating GRP78 and inhibiting the development of triple-negative breast cancer (TNBC). COX-2-IN-55 can also downregulate the levels of angiogenic markers VEGF-α and IL-8, inhibiting the formation of microvessels[1].

IC50 & Target

Caspase 3

 

VEGFR1

 

体外研究
(In Vitro)

COX-2-IN-55 (compound 1) 抑制 MDA-MB-231 细胞、MDA-MB-468 细胞、4T1 细胞、T47D 细胞和 MCF-7 细胞的活力,EC50 分别为 14.99 μM,14.26 μM,11.23 μM,17.3 μM,和 25.02 μM[1]

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

体内研究
(In Vivo)

COX-2-IN-55 (25 mg/kg/天,50 mg/kg/天;po;28 天) 在 MDA-MB-231 异种移植的 nu/nu 裸鼠模型中具有显著抗肿瘤特性,最高造成 85% 的肿瘤衰退[1]
100 mg/kg/天 COX-2-IN-55 剂量下,处理 48 天后对小鼠不产生显著的生化或组织学毒性[1]

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

分子量

486.51

Formula

C24H21F3N4O2S

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
  • 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:
COX-2-IN-55
目录号:
HY-171992
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