GSK-1070916  (Synonyms: GSK-1070916A)

GSK-1070916 (GMP) is GSK-1070916 (HY-70044) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with K_is of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A^[1][2].

GSK-1070916 (GMP) 强效抑制 Aurora B/INCENP 和 Aurora C/INCENP 激酶，K_i 分别为 0.38 和 1.45 nM，但对 Aurora A/TPX2 的抑制作用较弱，K_i 为 492 nM。GSK-1070916 (GMP) 还能抑制 FLT1、TIE2、SIK、FLT4 和 FGFR1，IC₅₀ 值分别为 42、59、70、74 和 78 nM。GSK-1070916 (GMP) 处理 A549 人肺癌细胞可产生强效的抗增殖作用 (EC₅₀=7 nM)^[1]。
GSK-1070916 (GMP) 可抑制一组肿瘤细胞系，并显示出可抑制所有细胞系中 HH3-S10 的磷酸化，平均 EC₅₀ 值范围为 8 至 118 nM^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

在植入人结肠肿瘤 (HCT116) 异种移植瘤的裸鼠中，单剂量腹腔注射 GSK-1070916 (GMP) 可剂量依赖性地抑制 HH3-S10 磷酸化。重复腹腔注射 GSK-1070916 (GMP) 对 8 种肿瘤类型中的 4 种 (肺癌，A549；结肠癌，HCT116；急性髓性白血病 (AML)，HL60；以及慢性髓性白血病，K562) 产生完全或部分抗肿瘤活性，对 8 种肿瘤类型中的 3 种 (结肠癌，Colo205；肺癌，H460；以及乳腺癌，MCF-7) 产生稳定效果，并对 8 种肿瘤类型中的 1 种 (结肠癌，SW620) 产生肿瘤生长延缓。每日服用 GSK-1070916 (GMP)通常耐受性良好^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

507.63

C₃₀H₃₃N₇O

942918-07-2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Adams ND, et al. Discovery of GSK-1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001.  [Content Brief]

  [2]. Hardwicke MA, et al. GSK-1070916, a potent Aurora B/C kinase inhibitor with broad antitumor activity in tissue culture cells and human tumor xenograft models. Mol Cancer Ther. 2009 Jul;8(7):1808-17.  [Content Brief]