Basic information Description In vitro In vivo Safety Related Supplier
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MLN-8237

Basic information Description In vitro In vivo Safety Related Supplier
MLN-8237 Basic information
MLN-8237 Chemical Properties
  • Boiling point:729.1±70.0 °C(Predicted)
  • Density 1.43±0.1 g/cm3(Predicted)
  • pka4.07±0.10(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. [1] 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.
MLN-8237(1028486-01-2)Related Product Information
MLN-8237SupplierMore
  • Company Name:Shanghai Boyle Chemical Co., Ltd.
  • Tel:
  • Email:sales@boylechem.com
  • Products Intro:Product Name:MLN-8237
    CAS:1028486-01-2
  •  
  • Company Name:J & K SCIENTIFIC LTD.
  • Tel:400-666-7788 010-82848833-
  • Email:jkinfo@jkchemical.com;market6@jkchemical.com
  • Products Intro:Product Name:MLN 8237 (Contain 10% DMSO)
    CAS:1028486-01-2
    Package:50Mg,5Mg
  •  
  • Company Name:Chembest Research Laboratories Limited
  • Tel:021-20908456-
  • Email:sales@BioChemBest.com
  • Products Intro:Product Name:Alisertib (MLN 8237)
    CAS:1028486-01-2
    Purity:98%+ Package:50mg;100mg;500mg;1g;5g;10g Remarks:C15972
  •  
  • Company Name:JinYan Chemicals(ShangHai) Co.,Ltd.
  • Tel:13817811078,021-50426030
  • Email:sales@jingyan-chemical.com
  • Products Intro:Product Name:MLN8237
    Purity:98%
  •  
  • Company Name:Nanjing Chemlin Chemical Co., Ltd
  • Tel:025-83697070-
  • Email:info@chemlin.com.cn
  • Products Intro:CAS:1028486-01-2
    Purity:98.00% Package:10g;500g;1kg;10kg
  •