| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S23294-5mg促销 |
≥98%(HPLC) | ￥598.00 ￥538.00 |
10 | - | - | - | - |
|
S23294-10mg促销 |
≥98%(HPLC) | ￥682.00 ￥612.00 |
10 | - | - | - | - |
|
S23294-25mg促销 |
≥98%(HPLC) | ￥736.00 ￥662.00 |
10 | - | - | - | - |
|
S23294-50mg促销 |
≥98%(HPLC) | ￥1180.00 ￥1060.00 |
5 | - | - | - | - |
|
S23294-100mg促销 |
≥98%(HPLC) | ￥1880.00 ￥1690.00 |
6 | - | - | - | - |
|
S23294-250mg促销 |
≥98%(HPLC) | ￥3200.00 ￥2880.00 |
1 | - | - | - | - |
|
| 产品描述： | ETP-45658 is a potent PI3K inhibitor, with IC50s of 22.0 nM, 39.8 nM, 129.0 nM and 717.3 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. ETP-45658 also can inhibit DNA-PK (IC50=70.6 nM) and mTOR (IC50=152.0 nM). ETP-45658 can be used for the research of cancer | ||||||||||||||||||||
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| 靶点： | PI3Kα：22.0 nM (IC50)；PI3Kδ：39.8 nM (IC50)；PI3Kβ：129.0 nM (IC50)；PI3Kγ：717.3 nM (IC50)；mTOR：152.0 nM (IC50)；DNA-PK：70.6 nM (IC50);DNA-PK;PI3K;mTOR | ||||||||||||||||||||
| 体外研究： | ETP-45658 (10 μM; 4 h) decreases in the phosphorylation of FOXO3a, Gsk3-β and p70 S6K in U2OS cells. ETP-45658 inhibits the proliferation of MCF7, PC3, 786-O, HTC116, and U251 cells, with EC50s of 0.48 μM, 0.49 μM, 2.62 μM, 3.53 μM, and 5.56 μM, respectively. ETP-45658 (10 μM; 24 h) induces a clear G1 arrest of PC3 cells. ETP-45658 inhibits the mutant PI3Kα proteins, H1047R and E545K, with IC50s of 16.8 nM and 13.1 nM, respectively. ETP-45658 (5 nM-11.1 μM; 1 h) induces a dose-dependent increase of GFP-FOXO nuclear translocation in U2foxRELOC cells. ETP-45658 (10 μM; 1 h) decrease the expression of cyclin D1 and p-Akt on serine 473 in U2OS cells. |
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| 体内研究： | ETP-45658 (22.7 mg/kg) decreases the level of phosphorylated Akt on serine 473 in the mammary ducts of transgenic mice. | ||||||||||||||||||||
| 参考文献： | 1. Link W, et, al. Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases. J Biol Chem. 2009 Oct 9;284(41):28392-28400. 2. Hill R, et, al. A novel phosphatidylinositol 3-kinase (PI3K) inhibitor directs a potent FOXO-dependent, p53-independent cell cycle arrest phenotype characterized by the differential induction of a subset of FOXO-regulated genes. Breast Cancer Res. 2014 Dec 9;16(6):482. |
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| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 备注： | ETP-45658 是一种有效的 PI3K 抑制剂，抑制 PI3Kα，PI3Kδ，PI3Kβ 和 PI3Kγ的 IC50 值分别为 22.0 nM，39.8 nM，129.0 nM 和 717.3 nM。ETP-45658 还可以抑制 DNA-PK (IC50=70.6 nM) 和 mTOR (IC50=152.0 nM)。 | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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