1. MAPK/ERK Pathway Stem Cell/Wnt
  2. ERK
  3. ADTL-EI1712

ADTL-EI1712 是一种口服有效的 ERK1ERK5 的选择性双靶点抑制剂,1 μM 时对 ERK1/5 的抑制率分别为 93.54% 和 89.35%。ADTL-EI1712 可诱导调节性细胞死亡(一种依赖于基因编码机制激活的细胞死亡形式),以克服体外和体内特定癌细胞的补偿机制。

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ADTL-EI1712 Chemical Structure

ADTL-EI1712 Chemical Structure

CAS No. : 2414916-45-1

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查看 ERK 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ADTL-EI1712 is a potent, orally active, and selective dual-target inhibitor of ERK1 and ERK5, inhibition rates of ERK1/5 at 1 μM are 93.54% and 89.35%, respectively. ADTL-EI1712 can induce regulated cell death, a form of cell death that relies on the activation of genetically encoded machinery, to overcome compensatory mechanism in specific cancer cells in vitro and in vivo[1].

体外研究
(In Vitro)

ADTL-EI1712 对 HL-60、MKN-74 和 HeLa 细胞具有抗增殖活性,IC50 值分别为 1.26+0.57、2.55+0.66、>50 μM[1]
ADTL-EI1712 (0.5 μM, 24 h) 可在 MKN-74 细胞中诱导受调节的细胞死亡并伴有自噬 (autophagy)[1]

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

体内研究
(In Vivo)

ADTL-EI1712 (50 mg/kg,口服,每天一次,持续16天) 显著抑制 HL-60 和 MKN-74 细胞异种移植小鼠模型中的肿瘤体积,而 HeLa 细胞组的抗肿瘤作用要弱得多< sup>[1]。

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

分子量

505.44

Formula

C22H18Cl2N4O2S2

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

ADTL-EI1712 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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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HY-138215
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