貨號	規格	價格	上海	北京	武漢	南京
S80328-5mg	99.6%	￥120.00 S80328-5mg ￥120.00 現貨	6 6	-	-	-
S80328-10mg	99.6%	￥200.00 S80328-10mg ￥200.00 現貨	6 6	-	-	-
S80328-25mg	99.6%	￥380.00 S80328-25mg ￥380.00 現貨	6 6	-	-	-
S80328-50mg	≥99%	￥570.00 S80328-50mg ￥570.00 2-3天	0 貨期：2-3天	-	-	-
S80328-100mg	≥99%	￥910.00 S80328-100mg ￥910.00 2-3天	0 貨期：2-3天	-	-	-

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產品介紹

PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM in a cell-free assay.

產品描述：

PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM in a cell-free assay.

靶點：

IC50: 0.22 μM (BRD4);Apoptosis;EpigeneticReaderDomain;Autophagy

體內研究：

PFI-1 administrated (1 mg/kg, i.v.) in the rat results in the volume of distribution of 1 L/kg, the plasma clearance of 18 mL/min/kg and half-life of 1 hour. PFI-1 oral dosed (2 mg/kg) in the rat results in the oral bioavailability as low as 32%. PFI-1 administrated (2 mg/kg, s.c.) in the mouse results in a Cmax of 58 ng/mL with a Tmax of 1 h and a half-life of approximately 2 hours

參考文獻：

1. Picaud S, et al. PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains. Cancer Res. 2013 May 21. [Epub ahead of print] 2. Fish PV, et al. Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. J Med Chem. 2012 Nov 26;55(22):9831-7. 3. Cheng Z, et al. Inhibition of BET bromodomain targets genetically diverse glioblastoma. Clin Cancer Res. 2013 Apr 1;19(7):1748-59. 4. Kate E Lines, et al. Epigenetic modifiers reduce proliferation of human neuroendocrine tumour cell lines. Endocrine Abstracts (2013) 31 P149

溶解性：

DMSO : 33.33 mg/mL (95.94 mM; Need ultrasonic)

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.879 ml	14.393 ml	28.786 ml
5 mM	0.576 ml	2.879 ml	5.757 ml
10 mM	0.288 ml	1.439 ml	2.879 ml
50 mM	0.058 ml	0.288 ml	0.576 ml

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。

參考文獻

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