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ON 146040
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
ON 146040图片
CAS NO:1404231-34-0
包装与价格：
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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)。
Cas No.1404231-34-0
Canonical SMILESCN(CC1)CCN1C(C=C2)=CC=C2NC3=NC(S/C(C(N4)=O)=C\C5=CC=C([N+]([O-])=O)C=C5)=C4C=N3
分子式C24H23N7O3S
分子量489.55
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.