产品
编 号:F086942
分子式:C20H23BCl2N2O9
分子量:517.12
纯 度:≥98%
产品类型
10mM*1mL in DMSO
456
In-stock
结构图
CAS No: 1239908-20-3
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产品详情
生物活性:
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.
体内研究:
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.
体外研究:
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.