TAK-960

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TAK-960 是一种口服生物可利用的选择性 Plk 抑制剂，对 Plk1、Plk2 和 Plk3 的 IC50 值分别为 0.8、16.9 和 50.2 nM。

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.(In Vitro):TAK-960 treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3). TAK-960 (2-1000 nM; 72 hours) inhibits proliferation of multiple cancer cell lines, with mean EC50 values ranging from 8.4 to 46.9 nM, but not in nondividing normal cells.TAK-960 (8?nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells.(In Vivo):TAK-960 exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts.In animal models, TAK-960 (p.o.) increases pHH3 in a dose-dependent manner and significantly inhibits the growth of HT-29 colorectal cancer xenografts.

TAK-960 treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3). TAK-960 (2-1000 nM; 72 hours) inhibits proliferation of multiple cancer cell lines, with mean EC50 values ranging from 8.4 to 46.9 nM, but not in nondividing normal cells. TAK-960 (8?nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells. Cell Viability AssayCell Line:HT-29, HCT116, COLO320DM, HCT-15, RKO, SW480, K-562….Hela, DU 145 cells Concentration:2-1000 nM Incubation Time:72 hours Result:Inhibited proliferation of human cancer cell lines regardless of TP53 and KRAS mutation and MDR1 expression status.

TAK-960 exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts.In animal models, TAK-960 (p.o.) increases pHH3 in a dose-dependent manner and significantly inhibits the growth of HT-29 colorectal cancer xenografts. Animal Model:nude mice or SCID mice (bearing HCT116, PC-3, BT474, A549, NCI-H1299, NCI-H1975, A2780, and MV4-11 cells)Dosage:10 mg/kg Administration:P.o.; once daily for 2 weeks Result:Substantial antitumor activity and good tolerability.

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Cell Cycle/DNA Damage

PLK

PLK

Cancer

Acute myeloid leukaemia; Solid tumours

1137868-52-0

561.6

C27H34F3N7O3

>98% (HPLC)

DMSO:35 mg/mL (62.32 mM)

COc1cc(C(=O)NC2CCN(C)CC2)c(F)cc1Nc1ncc2N(C)C(=O)C(F)(F)CN(C3CCCC3)c2n1

4-((9-cyclopentyl-77-difluoro-5-methyl-6-oxo-6789-tetrahydro-5H-pyrimido[45-b][14]diazepin-2-yl)amino)-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide

(-20℃)

With Ice Pack

≥ 2 years