生物活性

• 靶点

  Abl IC50:1nM

  Src IC50:1.2nM

• 描述Bosutinib is selective for Src over non-Src family kinases with an IC50 of 1.2 nM, and potently inhibits Src-dependent cell proliferation with an IC50 of 100 nM. Bosutinib significantly inhibits the proliferation of Bcr-Abl-positive leukemia cell lines KU812, K562, and MEG-01 but not Molt-4, HL-60, Ramos, and other leukemia cell lines, with IC50 of 5 nM, 20 nM and 20 nM, respectively, more potently than that of STI-571. Similar to STI-571, Bosutinib displays antiproliferative activity against the Abl-MLV-transformed fibroblasts with IC50 of 90 nM. Bosutinib ablates tyrosine phosphorylation of Bcr-Abl and STAT5 in CML cells and of v-Abl expressed in fibroblasts at the concentration of ~50 nM, 10-25 nM and 200 nM, respectively, leading to the Bcr-Abl downstream signaling inhibition of Lyn/Hck phosphorylation. Although unable to inhibit the proliferation and survival of breast cancer cells, Bosutinib significantly decreases the motility and invasion of breast cancer cells with IC50 of ~250 nM, involved with an increase in cell-to-cell adhesion and membrane localization of β-catenin.
• 细胞研究
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  23132-87	-	Growth Inhibition Assay	-	IC50=15.8495 μM	SANGER
  5637	-	Growth Inhibition Assay	-	IC50=1.13803 μM	SANGER
  647-V	-	Growth Inhibition Assay	-	IC50=29.7003 μM	SANGER

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• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02551718	Acute Leukemia of Ambiguous Li... more >>neage Recurrent Adult Acute Lymphoblastic Leukemia Recurrent Adult Acute Myeloid Leukemia Recurrent Childhood Acute Lymphoblastic Leukemia Recurrent Childhood Acute Myeloid Leukemia Refractory Acute Myeloid Leukemia Refractory Adult Acute Lymphoblastic Leukemia Refractory Childhood Acute Lymphoblastic Leukemia Collapse <<	Not Applicable	Recruiting	-	United States, Washington ... more >> Fred Hutch/University of Washington Cancer Consortium Recruiting Seattle, Washington, United States, 98109 Contact: Pamela S. Becker    206-616-1589    pbecker@u.washington.edu    Principal Investigator: Pamela S. Becker Collapse <<
  NCT03610971	Chronic Phase Chronic Myeloid ... more >>Leukemia Chronic Myeloid Leukemia, Chronic Phase Collapse <<	Phase 2	Not yet recruiting	January 2022	United States, Florida ... more >> H. Lee Moffitt Cancer Center and Research Institute Not yet recruiting Tampa, Florida, United States, 33612 Contact: Anthony McLaughlin    813-745-5941    anthony.mclaughlin@moffitt.org    Contact: Kendra Sweet, M.D.    813-745-8986    kendra.sweet@moffitt.org    Principal Investigator: Kendra Sweet, M.D. Collapse <<
  NCT03746054	Chronic Myeloid Leukemia (CML)	Phase 3	Not yet recruiting	March 2023	-

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