MLN8237 (Alisertib)Catalog No. A10004

Quick Overview

MLN8237 (Alisertib) 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..
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MLN8237 (Alisertib)

MLN8237 (Alisertib)  Citations(4)
  • Kimura M, .et al. Aurora A regulates the architecture of the Golgi apparatus, Exp Cell Res, 2018, Jun 1;367(1):73-80 PMID: 29571950
  • Jing Wang, .et al. The Aurora-A–Twist1 axis promotes highly aggressive phenotypes in pancreatic carcinoma, J Cell Sci, 2017, Mar 15; 130(6): 1078–1093 PMID: 28167680
  • Lessing D, .et al. A high-throughput small molecule screen identifies synergism between DNA methylation and Aurora kinase pathways for X reactivation, Proc Natl Acad Sci U S A, 2016, Dec 13;113(50):14366-14371 PMID: 28182563
  • Jennifer M. Sahni, .et al. Bromodomain and Extraterminal Protein Inhibition Blocks Growth of Triple-negative Breast Cancers through the Suppression of Aurora Kinases, J Biol Chem, 2016, Nov 4; 291(45): 23756–23768 PMID: 27650498
  • Product Information
    Catalog Num A10004
    M. Wt 518.9
    Formula C27H20ClFN4O4
    Solubility DMSO>44mg/mL Water <1mg/mL Ethanol <1mg/mL
    Purity >98%
    Storage at -20°C 3 years Powder
    CAS No. 1028486-01-2
    Synonyms N/A
    Chemical Name 4-[[9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid
    SMILES Code COC1=C(C(=CC=C1)F)C2=NCC3=CN=C(N=C3C4=C2C=C(C=C4)Cl)NC5=CC(=C(C=C5)C(=O)O)OC

    Biological activity
    Introduction
    MLN8237 (Alisertib) 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..
    Solubility
    Solubility (25C) * In vitro DMSO 27 mg/mL (52.03 mM)
    Water <1 mg/mL (<1 mM)
    Ethanol <1 mg/mL (<1 mM)
    In vivo 15% Captisol 30 mg/mL
    * <1 mg/ml means slightly soluble or insoluble.
    * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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    High Purity Kinase Inhibitors on Signaling Pathways

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