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GSK1070916
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK1070916图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
200mg电议

产品介绍
GSK1070916 是一种有效的、选择性的 ATP 竞争性 Aurora B 和 aurora C 抑制剂,Kis 分别为 0.38 和 1.5 nM,比 Aurora A 选择性高 250 倍以上。

Cell experiment:

A panel of tumor cell lines are plated in 96-well plates in the recommended growth media and incubated at 37℃ in 5% CO2 overnight. The following day, the cells are treated with serial dilutions of GSK-1070916. At this time, one set of cells is treated with CellTiter-Glo for a time equal to 0 (T=0) measurement. Following a 6- to 7-d incubation with compound, cell proliferation is measured using the CellTiter-Glo reagent[2].

Animal experiment:

Mice: Tumors are initiated by injection of tumor cell suspensions (A549, SW620, HCT116, H460, MCF-7, HL60, K562) or tumor fragments (Colo205) s.c. into nude (A549, SW620, HCT116, H460, MCF-7, HL60, and Colo205) or severe combined immunodeficient (SCID; K562) mice. When the tumors reach a volume of 80 to 200 mm3, the mice are randomized into groups of 5 to 10 mice per group. GSK-1070916 is administered at 25, 50, or 100 mg/kg once daily for 5 consecutive days-on, 2d-off, schedule for two (Colo205 and HL60) or three (A549, SW620, HCT116, H460, MCF-7, K562) cycles. Tumors are measured twice weekly[2].

产品描述

GSK1070916 is a potent and selective inhibitor of Aurora B/C Kinase with Ki values of 0.38nM and 1.5nM, respectively [1].

GSK1070916 is a reversible ATP-competitive inhibitor of Aurora B and Aurora C with Ki values of 0.38nM and 1.5nM, respectively. The SPA assay shows GSK1070916 has a good selectivity over Aurora A. It inhibits Aurora B with IC50 value of 5nM but 1259nM for Aurora A. It is also reported that treatment of GSK1070916 suppresses cell proliferation in A549 human lung cancer cells with EC50 value of 7nM. Moreover, both in vitro and in vivo assays demonstrate GSK1070916 can inhibit the phosphorylation of histone H3, which is a substrate of Aurora B. GSK1070916 can also suppress tumor growth in mice with HL-60 tumor xenografts [1].

References:
[1] Adams ND, Adams JL, Burgess JL, Chaudhari AM, Copeland RA, Donatelli CA, Drewry DH, Fisher KE, Hamajima T, Hardwicke MA, Huffman WF, Koretke-Brown KK, Lai ZV, McDonald OB, Nakamura H, Newlander KA, Oleykowski CA, Parrish CA, Patrick DR, Plant R, Sarpong MA, Sasaki K, Schmidt SJ, Silva DJ, Sutton D, Tang J, Thompson CS, Tummino PJ, Wang JC, Xiang H, Yang J, Dhanak D. Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001.