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產品描述： GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM. |
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靶點：
IC50: 10 nM(PDK1);PDK |
體內研究：
The efficacy of the PDK1 inhibitor (PDKi) GSK2334470 is tested in newborn BrafV600E::Pten?/?mice subjected to systemic administration of 4-HT. Twice weekly administration of PDK1 results in marked inhibition of pigmented lesions and concomitant melanomagenesis, as well as significant inhibition of lung metastases, seen by H&E staining-based quantification (~80%), and lymph node metastases as by S100 immunostaining, similar to the phenotype seen upon genetic ablation of Pdk1 |
參考文獻：
1. Najafov A, et al. Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. Biochem J.?2011 Jan 15;433(2):357-69. 2. Qi L, et al. PDK1-mTOR signaling pathway inhibitors reduce cell proliferation in MK2206 resistant neuroblastoma cells. Cancer Cell Int.?2015 Sep 29;15:91. 3. Scortegagna M, et al. Genetic inactivation or pharmacological inhibition of Pdk1 delays development and inhibits metastasis of Braf(V600E)::Pten(-/-) melanoma. Oncogene. 2014 Aug 21;33(34):4330-9. |
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溶解性：
DMSO : ≥ 50 mg/mL (108.09 mM) |
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保存條件：
-20℃ |
配置溶液濃度參考：
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1mg |
5mg |
10mg |
| 1 mM |
2.162 ml |
10.809 ml |
21.617 ml |
| 5 mM |
0.432 ml |
2.162 ml |
4.323 ml |
| 10 mM |
0.216 ml |
1.081 ml |
2.162 ml |
| 50 mM |
0.043 ml |
0.216 ml |
0.432 ml |
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| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
北京