ON 146040

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ON 146040 

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)。

ON 146040

ON 146040 Chemical Structure

CAS No. : 1404231-34-0

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生物活性

ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).

IC50 & Target[1]

PI3Kα

14 nM (IC50)

PI3Kδ

20 nM (IC50)

PI3Kγ

1 μM (IC50)

PI3Kβ

3 μM (IC50)

体外研究
(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. represents first dual pi3k and bcr-abl inhibitor that targets stat3 stat5 pathways. disrupts oncogenic activity of both by targeting upstream activators, including α δ isoforms as well wild type mutant bcr-abl. 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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

489.55

Formula

C24H23N7O3S
CAS 号

1404231-34-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Targeting oncogenic STAT3 and STAT5 signaling with on 146040, a small molecule inhibitor of PI3K α/δ and BCR-ABL.

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