2. PI3K/Akt/mTOR
  3. PDK-1
  4. PF-5177624

PF-5177624 是一种特异性强效的 PDK1 抑制剂，PDK1 是 PI3K/AKT 信号通路中的关键酶，在乳腺癌中经常失调。PDK1 在 T308 和其他底物处磷酸化 AKT，激活对肿瘤进展很重要的下游信号通路。PF-5177624 阻断 IGF-1 刺激的 PDK1 活性和下游 AKT 和 p70S6K 磷酸化，减少乳腺癌细胞的细胞增殖和转化。

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PF-5177624 Chemical Structure

PF-5177624 Chemical Structure

CAS No. : 1350821-45-2

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PF-5177624 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-5177624 is a specific and potent inhibitor of PDK1, a key enzyme in the PI3K/AKT signaling pathway that is frequently dysregulated in breast cancer. PDK1 phosphorylates AKT at T308 and other substrates, activating downstream signaling pathways that are important for tumor progression. PF-5177624 blocks IGF-1-stimulated PDK1 activity and downstream AKT and p70S6K phosphorylation, reducing cell proliferation and transformation in breast cancer cells[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 EC50
1800 nM
Compound: 24
Antiproliferative activity against human A549 cells after 72 hrs by resazurin reduction assay
Antiproliferative activity against human A549 cells after 72 hrs by resazurin reduction assay
[PMID: 22040023]
A549 IC50
50 nM
Compound: 24
Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human A549 cells after 2 hrs by ELISA
Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human A549 cells after 2 hrs by ELISA
[PMID: 22040023]
NCI-H460 EC50
700 nM
Compound: 24
Antiproliferative activity against human H460 cells after 72 hrs by resazurin reduction assay
Antiproliferative activity against human H460 cells after 72 hrs by resazurin reduction assay
[PMID: 22040023]
SK-OV-3 IC50
70 nM
Compound: 24
Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human SKOV3 cells after 2 hrs by ELISA
Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human SKOV3 cells after 2 hrs by ELISA
[PMID: 22040023]
分子量

488.52

Formula

C25H25FN8O2
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

PF-5177624 相关分类

  • 摩尔计算器

  • 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.

Keywords:

PF-51776241350821-45-2PF5177624PF 5177624PDK-13-Phosphoinositide-dependent protein kinase 1Inhibitorinhibitorinhibit

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