ON 146040 |
| カタログ番号GC36807 |
ON 146040 は、強力な PI3Kα および PI3Kδ (IC50 ≈14 および 20 nM、それぞれ) 阻害剤です。 ON 146040 は Abl1 も阻害します (IC50 < 150 nM)。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1404231-34-0
Sample solution is provided at 25 µL, 10mM.
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ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM). PI3Kα|14 nM (IC50)|PI3Kδ|20 nM (IC50)|PI3Kγ|1 μM (IC50)|PI3Kβ|3 μM (IC50)|Abl1|150 nM (IC50)
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[1].
[1]. Targeting oncogenic STAT3 and STAT5 signaling with on 146040, a small molecule inhibitor of PI3K α/δ and BCR-ABL.
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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