A Plk1 inhibitor
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MLN0905

Item No. 31115

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[5-[3-(dimethylamino)propyl]-2-methyl-3-pyridinyl]amino]-5,7-dihydro-9-(trifluoromethyl)-6H-pyrimido[5,4-d][1]benzazepine-6-thione
CAS Number
1228960-69-7
Molecular Formula
C24H25F3N6S
Formula Weight
486.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
SMILES
FC(F)(F)C1=CC=C2C(NC(CC3=CN=C(NC4=C(C)N=CC(CCCN(C)C)=C4)N=C32)=S)=C1
InChi Code
InChI=1S/C24H25F3N6S/c1-14-19(9-15(12-28-14)5-4-8-33(2)3)31-23-29-13-16-10-21(34)30-20-11-17(24(25,26)27)6-7-18(20)22(16)32-23/h6-7,9,11-13H,4-5,8,10H2,1-3H3,(H,30,34)(H,29,31,32)
InChi Key
CODBZFJPKJDNDT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    MLN0905 is an inhibitor of polo-like kinase 1 (Plk1; IC50 = 2 nM).1 It inhibits 95% of Plk1 activity but also inhibits the activity of 10 additional kinases by greater than or equal to 90% in a panel of 359 kinases at 1 µM. MLN0905 reduces phosphorylation of histone H3 at serine 10 (H3S10Ph), a marker of cell cycle arrest at prometaphase, in HT-29 colorectal cancer cells (EC30 = 9 nM). It inhibits proliferation in a panel of six human lymphoma cell lines with IC50 values ranging from 3.2 to 24 nM.2 MLN0905, alone or in combination with rituximab, increases survival in an OCI LY-19 metastatic lymphoma mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Duffey, M.O., Vos, T.J., Adams, R., et al. Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of polo-like kinase 1 (MLN0905). J. Med. Chem. 55(1), 197-208 (2012).

    2. Shi, J.Q., Lasky, K., Shinde, V., et al. MLN0905, a small-molecule PLK1 inhibitor, induces antitumor responses in human models of diffuse large B-cell lymphoma. Mol. Cancer Ther. 11(9), 2045-2053 (2012).