TAK-960A Plk inhibitor

TAK-960 (CAS 1137868-52-0)

TAK-960 | CAS 1137868-52-0 is rated 5.0 out of 5 by 1.
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Application: A Plk inhibitor
CAS Number: 1137868-52-0
Purity: >98%
Molecular Weight: 561.6
Molecular Formula: C27H34F3N7O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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TAK-960 has shown activity in several tumor cell lines including those that express multi-drug resistant protein 1 (MDR1). Consistent with PLK1 inhibition, TAK-960 treatment gives rise to accumulation of G2/M cells, aberrant "polo" mitosis morphology, and increases phosphorylation of histone H3 (pHH3). TAK-960 inhibits proliferation of multiple cancer cell lines, with mean EC50 values ranging from 8.4 to 46.9 nM. TAK-960 is an inhibitor of Plk.

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mg/mL).
Storage :
Store at -20° C
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.62 (Predicted)
IC50 :
Plk: IC50 = 2 nM (human); HT-29: EC5050 = 3 nM (human)
pK Values :
pKa: 13.21 (Predicted), pKb: 8.64 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
53357478
MDL Number :
MFCD22420821
SMILES :
CN1CCC(CC1)NC(=O)C2=CC(=C(C=C2F)NC3=NC=C4C(=N3)N(CC(C(=O)N4C)(F)F)C5CCCC5)OC

Download SDS (MSDS)

Certificate of Analysis

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TAK-960  Product Citations

See how others have used TAK-960. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 29344898  2018. Methods Mol. Biol. 1711: 351-398.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Nair et al Nair et al. (PubMed ID 26236920) found that the kinase 1 (PLK-1) inhibitor TAK-960 induced apoptosis in sarcoma cell lines via down-regulation of Mcl-1 and PLK1 by siRNA. -SCBT Publication Review
Date published: 2015-05-29
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