Imatinib (STI571) 是一种口服生物可用的酪氨酸激酶抑制剂，可选择性抑制 BCR/ABL，v-Abl，PDGFR，c-kit 激酶活性。Imatinib (STI571) 靠近 ATP 结合位点结合，将其锁定在封闭或自我抑制的构象中，因此半竞争性抑制蛋白质的酶活性。Imatinib 还抑制 SARS-CoV 和 MERS-CoV。- 高纯度，全球文献引用。

Jul 1, 2002 · The best compound from this series was a methylpiperazine derivative that was originally named STI571 (imatinib, now known as Glivec or Gleevec), which was selected as the most promising candidate ...

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.

Apr 1, 2002 · 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 ...

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.

Oct 3, 2003 · 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 chromosom …

Oct 3, 2003 · 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. The Philadelphia chromosome occurs in 95% of people with chronic myeloid leukemia.

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. Results of clinical trials to date have demonstrated the crucial role of the bcr-abl tyrosine ...

Sep 3, 2024 · 体外：Imatinib (STI571) 抑制 c-Kit 自磷酸化、MAPK 激活和 Akt 激活，而不改变 c-kit、MAPK 或 Akt 的总蛋白水平。对这些作用产生 50% 抑制的浓度约为 100 nM [1] 。 伊马替尼 (STI571) 非常有效（体外 IC 50 为 25 nM) 对抗引起慢性粒

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.