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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规格 价格 是否有货 数量
5 mg ¥2790
3 - 4 周
10 mg ¥4770
3 - 4 周
25 mg 现货 3 - 4 周
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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].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HeLa IC50
> 50 μM
Compound: 22ac; ADTL-EI1712
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs
[PMID: 32078308]
HL-60 IC50
1.26 μM
Compound: 22ac; ADTL-EI1712
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability measured after 24 hrs
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability measured after 24 hrs
[PMID: 32078308]
MKN-74 IC50
2.55 μM
Compound: 22ac; ADTL-EI1712
Antiproliferative activity against human MKN74 cells assessed as reduction in cell viability measured after 24 hrs
Antiproliferative activity against human MKN74 cells assessed as reduction in cell viability measured after 24 hrs
[PMID: 32078308]
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
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  • 稀释计算器

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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:
ADTL-EI1712
目录号:
HY-138215
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