ON 146040

产品说明书

Print
Chemical Structure| 1404231-34-0 同义名 : -
CAS号 : 1404231-34-0
货号 : A464452
分子式 : C24H23N7O3S
纯度 : 99%+
分子量 : 489.55
MDL号 : MFCD28167819
存储条件:

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 In biochemical assays, ON 146040 inhibits PI3Kα and PI3Kδ isoforms (IC50≈14 and 20 nM, respectively) with minimal impact on PI3Kβ and PI3Kγ isoforms (IC50≈3 and 1 μM, respectively). ON 146040 also inhibits Abl1 and several mutant variants of this kinase (IC50<150 nM), except for the T315I mutant. Serving as the first dual PI3K and BCR-ABL inhibitor, ON 146040 targets the STAT3 and STAT5 pathways. It disrupts the oncogenic activity of STAT3 and STAT5 by targeting upstream activators, including PI3K α and δ isoforms, as well as wild-type and mutant BCR-ABL. ON 146040 exhibits high potency in eliminating hematologic tumor cells with IC50 values ranging from 150 to 1,000 nM. Treatment with ON 146040 results in down-regulation of STAT3 and STAT5 phosphorylation in leukemia and myeloma cells [1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.21mL

2.04mL

1.02mL

20.43mL

4.09mL

2.04mL

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.