A selective inhibitor of polo-like kinase 1
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TAK-960

Item No. 17701

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(9-cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-2-fluoro-5-methoxy-N-(1-methyl-4-piperidinyl)-benzamide
CAS Number
1137868-52-0
Molecular Formula
C27H34F3N7O3
Formula Weight
561.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 20 mg/mlEthanol: 12 mg/ml
λmax
280, 330 nm
SMILES
CN1CCC(NC(C2=CC(OC)=C(NC3=NC=C(N(C)C(C(F)(F)CN4C5CCCC5)=O)C4=N3)C=C2F)=O)CC1
InChi Code
InChI=1S/C27H34F3N7O3/c1-35-10-8-16(9-11-35)32-24(38)18-12-22(40-3)20(13-19(18)28)33-26-31-14-21-23(34-26)37(17-6-4-5-7-17)15-27(29,30)25(39)36(21)2/h12-14,16-17H,4-11,15H2,1-3H3,(H,32,38)(H,31,33,34)
InChi Key
GWRSATNRNFYMDI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $69

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    5 mg

    $297

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    10 mg

    $461

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    50 mg

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    Product Description

    TAK-960 is an orally bioavailable, selective inhibitor of Plks with IC50 values of 0.8, 16.9, and 50.2 nM for Plk1, Plk2, and Plk3, respectively.1,2 It exhibits greater than 20-fold selectivity for Plk1 over FAK, MLCK, and the tyrosine protein kinase Fes, and has minimal activity against a panel of 282 other kinases.1,2 It inhibits the proliferation of various cancer cell lines, including MDR1-expressing tumors, and also prevents tumor growth in several human cancer cell xenograft models, including a disseminated model of AML- and MDR1-expressing hematological tumors.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hikichi, Y., Honda, K., Hikami, K., et al. TAK-960, a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimens. Mol. Cancer Ther. 11(3), 700-709 (2012).

    2. Nie, Z., Feher, V., Natala, S., et al. Discovery of TAK-960: An orally available small molecule inhibitor of polo-like kinase 1 (PLK1). Bioorg. Med. Chem. Lett. 23(12), 3662-3666 (2013).