| CAS NO: | 1374996-60-7 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| Cas No. | 1374996-60-7 |
| 化学名 | 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 |
| 分子式 | C20H8N12O2 |
| 分子量 | 448.36 |
| 溶解度 | ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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: |
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