化合物XL228 T17267

Product Introduction
Bioactivity


英文名: XL228

描述: XL228 是一种多靶点酪氨酸激酶抑制剂，对 Bcr-Abl、Aurora A、IGF-1R、Src 和 Lyn 的 IC50 分别为 5、3.1、1.6、6.1和 2 nM。

体外活性: XL228 inhibits phosphorylation of BCR-ABL and its substrate STAT5 in K562 cells in vitro (IC50s: 33 and 43 nM, respectively). XL228 eliminates the phosphorylation of Aurora A and B at concentrations above 10 nM. XL228 displays a broad pattern of protein kinase inhibition, including the tyrosine kinases IGF1R, SRC, ABL, FGFR1-3, and ALK and the serine/threonine kinases Aurora A and Aurora B. Approximately 30% of the lines demonstrate XL228 IC50 values of <100nM in viability assays, including many lines with characterized ALK or FGFR mutations or amplifications [2][3].

体内活性: 单剂量药效学研究表明，XL228对K562异种移植瘤中BCR-ABL信号传导具有强大的影响。当XL228的血浆浓度达到3.5 μM时，BCR-ABL的磷酸化水平降低了50%；在0.8 μM的血浆浓度下，phospho-STAT5的减少程度与此相仿 [3]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 83.33 mg/mL (190.45 mM)


关键字: Inhibitor | Bcr-Abl | Aurora Kinase | XL 228 | XL-228 | Src | IGF-1R | XL228 | inhibit

相关产品: PD168393 | GIP (human) acetate | GSK1904529A | AVJ16 | Ginsenoside Rg5 | Chromeceptin | PQ401 | Ceritinib | AG1024 | Dusigitumab

相关库: Drug Repurposing Compound Library | Anti-Cancer Metabolism Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Pancreatic Cancer Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途