貨號	規格	價格	上海	北京	武漢	南京
S82540-2mg	99.7%	￥200.00 S82540-2mg ￥200.00 現貨	3 3	-	-	-
S82540-5mg	99.7%	￥350.00 S82540-5mg ￥350.00 現貨	5 5	-	-	-
S82540-10mg	99.7%	￥650.00 S82540-10mg ￥650.00 現貨	6 6	-	-	-
S82540-50mg	99.7%	￥1350.00 S82540-50mg ￥1350.00 現貨	3 3	-	-	-
S82540-100mg	≥99%	￥2280.00 S82540-100mg ￥2280.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM

產品描述：

Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM

靶點：

IC50: 3.4 nM (20S proteasome β5), 31 nM (20S proteasome β1), 3500 nM (20S proteasome β2);Proteasome;?Autophagy

體外研究：

Ixazomib citrate (MLN9708; 0.20-3.20 μM) inhibits the cell growth of both cell lines effectively in a time- and dose-dependent manner. Ixazomib induces cell cycle arrest in MG-63 and Saos-2 cells. Ixazomib induces apoptosis mainly through the caspases pathway and requires the activation of both caspase8 and caspase9. Ixazomib treatment increases the levels of pro-apoptotic proteins and down regulates the anti-apoptotic proteins that control MOMP. Ixazomib treatment induces the release of Cytc, Smac, OMI from mitochondria and decreases the protein levels of XIAP. Ixazomib inhibits the invasion ability of MG-63 and Saos-2 cells and decreases both the expression and secretion levels of MMP2/9.Ixazomib citrate (MLN9708; 12 nM) shows inhibitory activity against C-L and T-L proteasome activities. Treatment of H929 and MM.1S MM cells with Ixazomib triggers a marked increase in proteolytic cleavage of poly(ADP) ribose polymerase (PARP), a signature event during apoptosis. Ixazomib induces cleavage of caspase-3, an upstream activator of PARP. Ixazomib induces eIf2-α kinase activity and protein levels of Bip and CHOP/GADD153. Ixazomib blocks BMSCs-induced MM cell proliferation, inhibits in vitro capillary tubule formation, and target NF-κB

體內研究：

Ixazomib citrate (MLN9708; 11 mg/kg) significantly inhibits MM tumor growth and prolongs survival in the human plasmacytoma MM.1S xenograft mouse model. The blood chemistry profiles of Ixazomib-treated mice show normal levels of creatinine, hemoglobin, and bilirubin. Ixazomib dramatically increases the number of cleaved-caspase-3 positive cells of the xenograft model

參考文獻：

1. Liu R, et al. A New Perspective for Osteosarcoma Therapy: Proteasome Inhibition by MLN9708/2238 Successfully Induces Apoptosis and Cell Cycle Arrest and Attenuates the Invasion Ability of Osteosarcoma Cells in Vitro. Cell Physiol Biochem. 2017 Jan 27;41(2 2. Chauhan D, et al. In vitro and in vivo selective antitumor activity of a novel orally bioavailable proteasome inhibitor MLN9708 against multiple myeloma cells. Clin Cancer Res. 2011 Aug 15;17(16):5311-21. 3. Kupperman E, et al. Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer. Cancer Res. 2010 Mar 1;70(5):1970-80.

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.934 ml	9.669 ml	19.338 ml
5 mM	0.387 ml	1.934 ml	3.868 ml
10 mM	0.193 ml	0.967 ml	1.934 ml
50 mM	0.039 ml	0.193 ml	0.387 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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