1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. Bcr-Abl

Bcr-Abl (Bcr-Abl酪氨酸激酶)

Bcr-Abl tyrosine-kinase inhibitors (TKI) are the first-line therapy for most patients with chronic myelogenous leukemia (CML). More than 90% of CML cases are caused by a chromosomal abnormality that results in the formation of a so-called Philadelphia chromosome. This abnormality is a consequence of fusion between the Abelson (Abl) tyrosine kinase gene at chromosome 9 and the break point cluster (Bcr) gene at chromosome 22, resulting in a chimeric oncogene (Bcr-Abl) and a constitutively active Bcr-Abl tyrosine kinase that has been implicated in the pathogenesis of CML. Compounds have been developed to selectively inhibit the tyrosine kinase.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-111874
    SNIPER(ABL)-039 Inhibitor
    SNIPER(ABL)-039,由 Dasatinib (ABL 抑制剂) 通过 linker 与 LCL161 衍生物 (IAP 配体) 组合而成,可有效降解 BCR-ABL 蛋白,DC50 为 10 nM。对 ABLcIAP1,cIAP2,XIAPIC50 分别为 0.54 nM,10 nM,12 nM 和 50 nM。
    SNIPER(ABL)-039
  • HY-126143
    CHMFL-ABL-039 Inhibitor
    CHMFL-ABL-039 是一种具有高效选择性的 Ⅱ 型野生型 ABL 激酶和耐药 V299L 突变型 BCR-ABL 激酶的抑制剂,IC50 值分别为 7.9 nM、27.9 nM。CHMFL-ABL-039 可用于慢性粒细胞白血病 (CML) 的研究。
    CHMFL-ABL-039
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