An Aurora A kinase inhibitor
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MLN8237

Item No. 13602

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxy-benzoic acid
CAS Number
1028486-01-2
Synonyms
  • Alisertib
Molecular Formula
C27H20ClFN4O4
Formula Weight
518.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mLDMF:PBS(pH 7.2)(1:1): 0.5 mg/mLDMSO: 1 mg/mL
λmax
225, 314 nm
SMILES
COC1=C(C(O)=O)C=CC(NC2=NC3=C(CN=C(C4=C(F)C=CC=C4OC)C5=CC(Cl)=CC=C53)C=N2)=C1
InChi Code
InChI=1S/C27H20ClFN4O4/c1-36-21-5-3-4-20(29)23(21)25-19-10-15(28)6-8-17(19)24-14(12-30-25)13-31-27(33-24)32-16-7-9-18(26(34)35)22(11-16)37-2/h3-11,13H,12H2,1-2H3,(H,34,35)(H,31,32,33)
InChi Key
ZLHFILGSQDJULK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $145

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    10 mg

    $253

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    Product Description

    MLN8237 is an inhibitor of Aurora A kinase (IC50 = 1 nM).1 It is selective for Aurora A over Aurora B kinase (IC50 = 396.5 nM).2 MLN8237 (50 nM) induces cell cycle arrest at the G2/M phase and chromosomal misalignment in HCT116 colon cancer cells. It inhibits tumor growth in a Calu-6 non-small cell lung cancer (NSCLC) mouse xenograft model when administered at a dose of 20 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sells, T.B., Chau, R., Ecsedy, J.A., et al. MLN8054 and alisertib (MLN8237): Discovery of selective oral Aurora A inhibitors. ACS Med. Chem. Lett. 6(6), 630-634 (2015).

    2. Manfredi, M.G., Ecsedy, J.A., Chakravarty, A., et al. Characterization of alisertib (MLN8237), an investigational small-molecule inhibitor of Aurora A kinase using novel in vivo pharmacodynamic assays. Clin. Cancer Res. 17(24), 7614-7624 (2011).

    Product Citations

    Li, T., Huang, T., Du, M., et al. Phosphorylation and chromatin tethering prevent cGAS activation during mitosis. Science (2021).