2002年7月1日 · A lead compound identified in a screen for inhibitors of protein kinase C was optimized to give a methyl-piperazine derivative that was originally named STI571 (imatinib, now known as Glivec or...

2018年7月8日 · 在2009年出版的一本名为《科学的艺术性和政治性》(The Art and Politics of Science)的书中， 小哈 回忆说，STI571是“迄今为止，展现癌症研究最基本问题的解决，会对癌症病人带来巨大益处的最好证据。

Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively [1 ...

STI571 (formerly CGP57148B), is an ABL-specific inhibitor of tyrosine kinase that, in preclinical studies, selectively killed BCR-ABL-containing cells in vitro and in vivo. Clinical studies have shown the potential of this specifically targeted therapy, and STI571 is emerging as an important new therapeutic agent for chronic myelogenous leukaemia.

2002年4月1日 · STI571 (Gleevec™, imatinib mesylate) exemplifies the successful development of a rationally designed, molecularly targeted therapy for the treatment of a specific cancer. This article reviews the identification of Bcr-Abl as a therapeutic target in chronic myelogenous leukemia and the steps in the development of an agent to inactivate this ...

2003年10月3日 · STI-571 (imatinib, Gleevec, Glivec, CGP 57148) is an inhibitor of the Abl group of protein-tyrosine kinases. One of these enzymes, the Bcr-Abl oncoprotein, results from the fusion of the BCR and ABL genes that result from the reciprocal chromosomal translocation that forms the Philadelphia chromosome.

2024年9月3日 · Imatinib (STI571) 是 v-Abl、c-Kit 的多靶点抑制剂，可抑制 Bcr/Abl、v-Abl、Tel/Abl、天然 PDGFβ 受体和 c-Kit，但它不抑制 Src 家族激酶、c-Fms、Flt3、EGFR 或多种其他酪氨酸激酶。

2003年10月3日 · STI-571 is a competitive inhibitor of Abl kinase with respect to ATP. Resistance to STI-571 is often the result of mutations in residues of the Bcr-Abl kinase that ordinarily bind to the drug. Inhibition of target protein kinases represents an emerging therapeutic strategy for the treatment of cancer.

STI571 (formerly CGP57148B), is an Abl-specific tyrosine kinase inhibitor that in preclinical studies selectively kills Bcr-Abl-containing cells in vitro and in vivo. The results of clinical studies have demonstrated the potential of molecularly targeted therapies, and STI571 is emerging as a new therapeutic agent for CML.

Therapeutic agent STI571 (signal transduction inhibitor number 571) is a rationally developed, potent, and selective inhibitor for abl tyrosine kinases, including bcr-abl, as well c-kit and the platelet-derived growth factor receptor tyrosine kinases.