Among these molecules, STI571, previously known as CGP57148B, a 2-phenylaminopyrimidine derivative, is among the most promising and selective inhibitors of Bcr-Abl tyrosine kinase activity.

• STI571以bcr-abl融合基因为靶向，抑制BCR-ABL酪氨酸激酶活性，它是通过阻断ATP在ABL激酶上的结合位置而发挥作用，抑制了ABL转移ATPA上的磷酸集团及基质蛋白磷酸化酪氨酸残基的能力，从而阻止了ABL引起的细胞增殖和抗凋亡所必需的能量信号的转导。