TAK-960 Inhibitor CAS No. 1137868-52-0

Cat. No.	Name	Size	Price	Add Cart
KI0488	TAK-960	5 mg	$800
KI0488	TAK-960	50 mg	$3100

Chemical Characteristic

Product Name	TAK-960
CAS No.	1137868-52-0
Molecular Weight	561.6
Formula	C₂₇H₃₄F₃N₇O₃
Chemical 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
Smiles	C(=O)(c1c(cc(c(c1)OC)Nc1nc2N(CC(C(=O)N(c2cn1)C)(F)F)C1CCCC1)F)NC1CCN(CC1)C
Chemical Structure

Biological activities

TAK-960 is a novel, potent and selective Polo-like kinase 1 (PLK1) inhibitor. The IC50 value of TAK-960 against PLK1 is 0.8 nM. TAK-960 also inhibits PLK2 and PLK3 with IC50 values of 16.9 and 50.2 nM, respectively. In vitro, TAK-960 causes concentration-dependent accumulation of HT-29 colorectal cancer cells in G2-M phase. TAK-960 treatment also causes aberrant polo mitosis morphology and increases phosphorylation of histone H3 (pHH3) in vitro. TAK-960 inhibits proliferation of multiple cancer cell lines (including colorectal cancer, prostate cancer, and lung cancer) with mean EC50 values ranging from 8.4 to 46.9 nM, but not in nondividing normal cells with EC50> 1,000 nM. In various models of human cancer xenografts ( including colorectal cancer, prostate cancer, breast cancer, lung cancer, ovary cancer, and myeloid leukemia), TAK-960 treatment (10 mg/kg) shows significant antitumor activity.^[1]

References

[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, 11(3): 700-709.

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