貨號	規(guī)格	價格	上海	北京	武漢	南京
S34237-5mg	≥98%	￥1200.00 S34237-5mg ￥1200.00 現(xiàn)貨	100 >10	-	-	-
S34237-10mg	≥98%	￥1800.00 S34237-10mg ￥1800.00 現(xiàn)貨	50 >10	-	-	-
S34237-25mg	≥98%	￥3600.00 S34237-25mg ￥3600.00 現(xiàn)貨	20 >10	-	-	-
S34237-100mg	≥98%	￥10800.00 S34237-100mg ￥10800.00 現(xiàn)貨	5 5	-	-	-

產(chǎn)品介紹

Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) 是一種有效的，具有口服活性的，可逆的非競爭性的選擇性的 γ-secretase 抑制劑，IC50 為 6.2 nM。Nirogacestat dihydrobromide 抑制 Notch 信號通路，同時最小化胃腸道毒性?？捎糜谘芯?Notch 受體依賴性腫瘤。

產(chǎn)品描述：

靶點：

Apoptosis;Gamma-secretase

體外研究：

The IC50 of Nirogacestat (PF-03084014) for γ-secretase enzyme inhibition in cell-free assay for Aβ production using detergent solubilized membranes derived from HeLa cells is determined to be 6.2 nM. When tested for inhibition of Notch receptor cleavage in cellular assays using HPB-ALL cells that harbor mutations in both the heterodimerization and PEST domains in Notch1, the cell IC50 is determined to be 13.3 nM. Nirogacestat causes a significant increase in caspase-3 activities in HPB-ALL and TALL-1 cells as well as an induction of cleaved PARP and cleaved caspase-3 after a 7-day treatment.

體內(nèi)研究：

Nirogacestat (PF-03084014) shows robust antitumor activity in this model on 14-day twice daily dosing. Tumor growth inhibition is dose dependent, with maximal tumor growth inhibition of ~92% obtained at high dose levels (150 mg/kg). In tumor growth inhibition studies where mice receive repetitive twice daily dosing for more than a week, Nirogacestat is well tolerated at dose levels below 100 mg/kg as no significant weight loss, morbidity, or mortality is observed. When the dose is increased to 150 mg/kg, however, mice have diarrhea and show weight loss (10-15%) approximately 10 days after compound administration. The body weight of treated animals usually returns to normal if dosing holidays are given, suggesting that the toxicity of Nirogacestat is reversible.

參考文獻(xiàn)：

1. Wei P, et al. Evaluation of selective gamma-secretase inhibitor PF-03084014 for its antitumor efficacy and gastrointestinal safety to guide optimal clinical trial design. Mol Cancer Ther. 2010 Jun;9(6):1618-28.

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.535 ml	7.675 ml	15.35 ml
5 mM	0.307 ml	1.535 ml	3.07 ml
10 mM	0.153 ml	0.767 ml	1.535 ml
50 mM	0.031 ml	0.153 ml	0.307 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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Nirogacestat dihydrobromide