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化学性质:
规格 | 10mM * 1 mL in DMSO5mg |
CAS | 1374996-60-7 |
别名 | N/A |
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) |
分子式 | C20H8N12O 2 |
分子量 | 448.36 |
溶解度 | ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide |
储存条件 | Store at -20°C |
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 |
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.
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原创作者:上海莼试生物技术有限公司
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