Name: MLN8237 (Alisertib)
Price: 220.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    The orally bioavailable agent, MLN8237 (also known as alisertib), is a potent small-molecule inhibitor of Aurora A kinase (AAK) which is overexpressed in several types of tumor and associated with oncogenesis and tumor progression. It was developed from its predecessor, MLN8054, in order to minimize the benzodiazepine-like effects seen with MLN8054. The inhibitory effect of MLN8237 is ATP-competitive, reversible and AAK-specific with an inhibition constant (Ki) of 0.43 nmol/L. MLN8237 is being investigated to treat advanced malignancies, due to its both in vitro and in vivo activities against a broad range of tumor types.
- Properties
  - Alternative Name
    
    4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid
    
    CAS Number
    
    1028486-01-2
    
    Molecular Formula
    
    C27H20ClFN4O4
    
    Molecular Weight
    
    518.92
    
    Appearance
    
    A solid
    
    Purity
    
    98.09%
    
    Solubility
    
    ≥25.95 mg/mL in DMSO; insoluble in H2O; insoluble in ETOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Dammert MA, Br?gelmann J, et al. "MYC paralog-dependent apoptotic priming orchestrates a spectrum of vulnerabilities in small cell lung cancer." Nat Commun. 2019 Aug 2; 10 (1): 3485. PMID:31375684
    2. Laura Tomino, Emily Bopp, et al. "Combinatorial BRD4 and AURKA inhibition is synergistic against preclinical models of Ewing sarcoma." Cancer reports. 11 February 2019.
    3. Shaon Parial. "Novel Interaction, Regulation of Phosphorylation and Mitotic Localization of Cell Division Cycle Associated Protein 7 (CDCA7)" York University. 2018.
    4. Teke K, Yilmaz H, et al. "Histopathologic and molecular comparative analyses of intravesical Aurora kinase-A inhibitor Alisertib with bacillus Calmette-Guérin on precancerous lesions of bladder in a rat model." Int Urol Nephrol. 2018 Jun 21. PMID:29931492
    5. Krulikas LJ, McDonald IM, et al. "Application of Integrated Drug Screening/Kinome
    Analysis to Identify Inhibitors of Gemcitabine-Resistant Pancreatic Cancer Cell Growth." SLAS Discov. 2018 May 1:2472555218773045. PMID:29742358
    6. Joshua Felgenhauer, Laura Tomino, et al. "Dual BRD4 and AURKA Inhibition is Synergistic against MYCN-amplified and nonamplified Neuroblastoma." bioRxiv.2018 Mar.5.
    7. Mathison A, Salmonson A, et al."Combined AURKA and H3K9 Methyltransferase Targeting Inhibits Cell Growth By Inducing Mitotic Catastrophe." Mol Cancer Res. 2017 Aug; 15 (8): 984-997. PMID:28442587

MLN8237 (Alisertib)

MLN8237 (Alisertib)

Background

We Also Recommend

Barasertib (AZD1152-HQPA)

VX-680 (MK-0457,Tozasertib)

ZM 447439