An inhibitor of Aurora A kinase
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MLN8054

Item No. 27340

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[9-chloro-7-(2,6-difluorophenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-benzoic acid
CAS Number
869363-13-3
Molecular Formula
C25H15ClF2N4O2
Formula Weight
476.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleEthanol: Slightly soluble
λmax
226, 310 nm
SMILES
O=C(O)C1=CC=C(NC2=NC(C(C=CC(Cl)=C3)=C3C(C4=C(F)C=CC=C4F)=NC5)=C5C=N2)C=C1
InChi Code
InChI=1S/C25H15ClF2N4O2/c26-15-6-9-17-18(10-15)23(21-19(27)2-1-3-20(21)28)29-11-14-12-30-25(32-22(14)17)31-16-7-4-13(5-8-16)24(33)34/h1-10,12H,11H2,(H,33,34)(H,30,31,32)
InChi Key
HHFBDROWDBDFBR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $42

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    5 mg

    $173

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    10 mg

    $322

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    25 mg

    $702

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    Product Description

    MLN8054 is an ATP-competitive inhibitor of Aurora A kinase (IC50 = 4 nM).1 It is selective for Aurora A over Aurora B, PKC, CaMKII, Cdk2E, CK2, LCK, PKA, Chk1, Chk2, Cdk1, and Plk1 (IC50s = 0.172-100 µM). MLN8054 induces cell cycle arrest at the G2/M phase and the formation of abnormal mitotic spindles in HCT116 colorectal and PC3 prostate cancer cells. It inhibits the growth of HCT116, SW480, DLD-1, MCF-7, MDA-MB-231, Calu-6, H460, SKOV3, and PC3 cancer cells (IC50s = 0.11-1.43 µM). MLN8054 (30 mg/kg) reduces tumor volume in HCT116 and PC3 mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Manfredi, M.G., Ecsedy, J.A., Meetze, K.A., et al. Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. Proc. Natl. Acad. Sci. USA 104(10), 4106-4111 (2007).