ChemicalBook > Product Catalog > Biochemical Engineering > Inhibitors > Cell Cycle > Aurora Kinase Inhibitors > MLN-8237
MLN-8237 Chemical Properties
- Boiling point:729.1±70.0 °C(Predicted)
- Density 1.43±0.1 g/cm3(Predicted)
MLN-8237 Usage And Synthesis
- DescriptionAlisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3.
- In vitroMLN8237 shows >200-fold higher selectivity for Aurora A than the structurally related Aurora B with an IC50 of 396.5 nM, and does not have any significant activity against 205 other kinases.  MLN8237 (0.5 μM) treatment inhibits the phosphorylation of Aurora A in MM1.S and OPM1 cells, without affecting the Aurora B mediated histone H3 phosphorylation. MLN8237 significantly inhibits cell proliferation in multiple myeloma (MM) cell lines with IC50 values of 0.003-1.71 μM. MLN8237 displays more potent anti-proliferation activity against primary MM cells and MM cell lines in the presence of BM stroma cells, as well as IL-6 and IGF-1 than against MM cells alone. MLN8237 (0.5 μM) induces 2- to 6-fold increase in G2/M phase in primary MM cells and cell lines, as well as significant apoptosis and senescence, involving the up-regulation of p53, p21 and p27, as well as PARP, caspase 3, and caspase 9 cleavage. In addition, MLN8237 shows strong synergistic anti-MM effect with dexamethasone, as well as additive effect with doxorubicin and bortezomib.MLN8237 (0.5 μM) treatment causes the inhibition of colony formation of FLO-1, OE19, and OE33 esophageal adenocarinoma cell lines, and induces a significant increase in the percentage of polyploid cells, and subsequently an increase in the percentage of cells in the sub-G1 phase, which can be further enhanced in combination with cisplatin (2.5 μM), involving the higher induction of TAp73β, PUMA, NOXA, cleaved caspase-3, and cleaved PARP as compared with a single-agent treatment.
- In vivoMLN8237 significantly reduces the tumor burden with tumor growth inhibition (TGI) of 42% and 80% at 15 mg/kg and 30 mg/kg, respectively, and prolongs the survival of mice compared with the control.
- Chemical PropertiesOff-White Solid
- UsesAn Aurora kinase inhibitor, used to treat patients with advanced solid tumors.
- Company Name:Shanghai Boyle Chemical Co., Ltd.
- Products Intro:Product Name:MLN-8237
- Company Name:J & K SCIENTIFIC LTD.
- Tel:400-666-7788 010-82848833-
- Products Intro:Product Name:MLN 8237 (Contain 10% DMSO)
- Company Name:Chembest Research Laboratories Limited
- Products Intro:Product Name:Alisertib (MLN 8237)
Purity:98%+ Package:50mg;100mg;500mg;1g;5g;10g Remarks:C15972
- Company Name:JinYan Chemicals(ShangHai) Co.,Ltd.
- Products Intro:Product Name:MLN8237
- Company Name:Nanjing Chemlin Chemical Co., Ltd
- Products Intro:CAS:1028486-01-2