| CAS NO: | 1374996-60-7 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 224.2 |
| Cas No. | 1374996-60-7 |
| Formula | C10H4N6O·C10H4N6O |
| Solubility | ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide |
| Chemical Name | 6H-indeno[1,2-ε]tetrazolo[1,5-b][1,2,4]triazin-6-one, compd. with 10H-indeno[2,1-ε]tetrazolo[1,5-b][1,2,4]triazin-10-one (1:1) |
| Canonical SMILES | O=C(C1=C2C=CC=C1)C(C2=N3)=NN4C3=NN=N4.O=C5C6=NC7=NN=NN7N=C6C8=C5C=CC=C8 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
References:
[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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