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。

XL228 is an inhibitor of multi-targeted tyrosine kinase (IC50s: 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src, and Lyn, respectively).

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].

Single-dose pharmacodynamics studies demonstrate that XL228 on BCR-ABL signaling in K562 xenograft tumors has a potent effect. At XL228 plasma concentrations of 3.5 μM, phosphorylation of BCR-ABL is decreased by 50%; a similar decrease in phospho-STAT5 occurred at 0.8 μM plasma concentration [3].

898280-07-4

C22H31N9O

437.54

DMSO:83.33 mg/mL (190.45 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years