TAK960
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:多种癌细胞系的IC50为8.4到46.9 nmol/L.
Polo样激酶1(PLK1)是一种丝氨酸/苏氨酸蛋白激酶,参与有丝分裂的关键进程.在各种人类癌症中,人PLK1过表达.PLK1水平升高与不良预后相关,使其成为抗癌治疗的重要靶标.TAK-960是PLK1的新型的\研究性的和口服可利用的强效选择性抑制剂.
体外实验:TAK-960引起G2-M期细胞积累\polo有丝分裂形态异常以及组蛋白H3磷酸化的增加.在多种癌细胞系中,TAK-960抑制增殖,平均EC50范围为8.4至46.9 nmol/L,但对非分裂的正常细胞没有作用[1].
在体实验:在动物模型中,TAK-960口服给药以剂量依赖的方式增加pHH3,显著抑制HT-29结直肠癌异种移植物的生长.针对多种肿瘤异种移植物,每日一次TAK-960治疗具有显著功效,包括阿霉素/紫杉醇耐受的异种移植模型和弥散性白血病模型[1].
临床试验:在晚期非血液系统恶性肿瘤成年患者中,TAK-960目前正在进行I期的评估.
参考文献:
[1] Hikichi Y, Honda K, Hikami K, Miyashita H, Kaieda I, Murai S, Uchiyama N, Hasegawa M, Kawamoto T, Sato T, Ichikawa T, Cao S, Nie Z, Zhang L, Yang J, Kuida K, Kupperman E. 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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 561.6 |
Cas No. | 1137868-52-0 |
Formula | C27H34F3N7O3 |
Solubility | ≥28.05 mg/mL in DMSO; insoluble in H2O; ≥12.3 mg/mL in EtOH |
Chemical Name | 4-((9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino)-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide |
SDF | Download SDF |
Canonical SMILES | CN1CCC(NC(C2=CC(OC)=C(NC3=NC=C(N(C(C(F)(F)CN4C5CCCC5)=O)C)C4=N3)C=C2F)=O)CC1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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