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  • KP372-1
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KP372-1

An Akt inhibitor

原价
¥1200-3050
价格
960-2440
KP372-1的二维码

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  • 货号: ajci15348
  • CAS: 1374996-60-7
  • 别名:
  • 分子式: C20H8N12O 2
  • 分子量: 448.36
  • 纯度: >98%
  • 溶解度: ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide
  • 储存: Store at -20°C
  • 库存: 现货

Background

IC50: 30-60 nM for thyroid cancer cells


KP372-1 is a specific Akt inhibitor.


The phosphatidylinositol 3' kinase (PI3K)/phosphatase, which is a key regulator of cell proliferation and survival, is mutated or activated in various cancers. Akt seems to be a key central node in this pathway and therefore is an promising target.


In vitro: A previous study found that KP372-1 could block signalling downstream of Akt in thyroid tumour cells, resulting in inhibition of cell proliferation and increased apoptosis [1]. Another study showed that KP372-1 directly inhibited the kinase activity of AKT, FLT3, and PDK1concentration-dependently. Western blot analyses indicated KP372-1 decreased the phosphorylation of AKT on both Ser(473) and Thr(308). Moreover, the treatment of AML cell lines with KP372-1 led to rapid generation of reactive oxygen species and stimulation of oxygen consumption. In addition, KP372-1 was able to induce pronounced apoptosis in AML cell lines and primary samples irrespective of their FLT3 status, but not in normal CD34(+) cells [2].


In vivo: Up to now, there is no animal in vivo data reported.


Clinical trial: So far, no clinical study has been conducted.

参考文献:
[1] Mandal, M.?,Kim, S.,Younes, M.N., et al. The Akt inhibitor KP372-1 suppresses Akt activity and cell proliferation and induces apoptosis in thyroid cancer cells. British Journal of Cancer 92(10), 1899-1905 (2005).
[2] Zeng, Z.?,Samudio, I.J.,Zhang, W., et al. Simultaneous inhibition of PDK1/AKT and Fms-like tyrosine kinase 3 signaling by a small-molecule KP372-1 induces mitochondrial dysfunction and apoptosis in acute myelogenous leukemia. Cancer Research 66(7), 3737-3746 (2006).

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