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ON 146040

CAS No. : 1404231-34-0

MCE 国际站：ON 146040

产品活性：ON 146040 是一种有效的 PI3Kα 和 PI3Kδ 抑制剂，IC₅₀ 分别约为 14 和 20 nM。ON 146040 也抑制 Abl1 (IC₅₀<150 nM)。

研究领域：PI3K/Akt/mTOR  |  Protein Tyrosine Kinase/RTK

作用靶点：PI3K  |  Bcr-Abl

In Vitro: In biochemical testing, ON 146040 inhibits PI3Kα/ PI3Kδ isoforms (IC₅₀≈14 and 20 nM, respectively) without having a major effect on PI3Kβ/ PI3Kγ isoforms (IC₅₀≈3 and 1 μM, respectively). ON 146040 is also found to inhibit Abl1 and several mutant versions of this kinase (IC₅₀<150 nM), although ON 146040 is not found to be active against the T315I mutant. ON 146040 represents the first dual PI3K and BCR-ABL inhibitor that targets the STAT3 and STAT5 pathways. ON 146040 disrupts the oncogenic activity of both STAT3 and STAT5 by targeting upstream activators, including PI3K α and δ isoforms as well as wild type and mutant BCR-ABL. ON 146040 is highly potent in killing hematologic tumor cells with IC₅₀ values in the 150 to 1,000 nM range. Following treatment with ON 146040, STAT3 and STAT5 phosphorylation are down-regulated in leukemia and myeloma cells.

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