Alisertib

• Description :

  Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity[1][2][3].

• Product Name Alternative :

  MLN 8237

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H312, H332

• Target :

  Apoptosis; Aurora Kinase; Autophagy

• Type :

  Reference compound

• Related Pathways :

  Apoptosis; Autophagy; Cell Cycle/DNA Damage; Epigenetics

• Applications :

  Cancer-Kinase/protease

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/Alisertib.html

• Purity :

  99.84

• Solubility :

  DMSO : 25 mg/mL (ultrasonic)

• Smiles :

  O=C(C1=CC=C(C=C1OC)NC2=NC=C3CN=C(C4=CC(Cl)=CC=C4C3=N2)C5=C(C=CC=C5F)OC)O

• Molecular Formula :

  C27H20ClFN4O4

• Molecular Weight :

  518.92

• Precautions :

  H302, H312, H332

• References & Citations :

  [1]Güllü G, et al. A novel Aurora-A kinase inhibitor MLN8237 induces cytotoxicity and cell-cycle arrest in multiple myeloma Blood June 24, 2010 vol. 115 no. 25 5202-5213.|[2]Sloane DA, et al. Drug-Resistant Aurora A Mutants for Cellular Target Validation of the Small Molecule Kinase Inhibitors MLN8054 and MLN8237 ACS Chem. Biol., 2010, 5 (6), pp 563-576.|[3]Bavetsias V, et al. Aurora Kinase Inhibitors: Current Status and Outlook. Front Oncol. 2015 Dec 21;5:278.|[4]Manfredi MG, et al. Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays.Clin Cancer Res. 2011 Dec 15;17 (24) :7614-7624.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 3

• Isoform :

  Aurora A; Aurora B

• CAS Number :

  [1028486-01-2]