TAK-960

• UNSPSC Description:

  TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts[1].

• Target Antigen:

  Polo-like Kinase (PLK)

• Type:

  Reference compound

• Related Pathways:

  Cell Cycle/DNA Damage

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/TAK-960.html

• Solubility:

  DMSO : 16.67 mg/mL (ultrasonic;warming;heat to 60°C)

• Smiles:

  O=C(NC1CCN(C)CC1)C2=CC(OC)=C(NC3=NC=C(N4C)C(N(C5CCCC5)CC(F)(F)C4=O)=N3)C=C2F

• Molecular Weight:

  561.60

• References & Citations:

  [1]Hikichi Y, 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. 2012 Mar;11(3):700-9.|[2]Inoue M, et al. PLK1 blockade enhances therapeutic effects of radiation by inducing cell cycle arrest at the mitotic phase. Sci Rep. 2015 Oct 27;5:15666.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  Phase 1

• CAS Number:

  1137868-52-0