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CTA 056 是一种 ITK(IL-2 诱导型 T 细胞激酶)抑制剂,IC50 为 0.1 μM。 CTA 056 选择性地靶向恶性 T 细胞并调节肿瘤细胞。 CTA 056 诱导细胞凋亡,是治疗 T 细胞白血病和淋巴瘤的潜在治疗剂。
Interleukin-2-inducible T-cell kinase (ITK) inhibitor (IC50 values are 0.1, 0.4 and 5 μM for ITK, BTK and ETK, respectively). Inhibits growth of cancer cells expressing ITK, including MOLT-4 and Jurkat cells in vitro. Induces apoptosis in Jurkat cells. Inhibits MOLT-4 xenograft tumor growth in mice.
Guo et al (2012) Molecular characteristics of CTA056, a novel interleukin-2-inducible T-cell kinase inhibitor that selectively targets malignant T cells and modulates oncomirs. Mol.Pharmacol. 82 938 PMID:22899868
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