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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 |
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溶解度 : | - | |
动物实验配方: |
生物活性 | |||
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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 | |||
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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 |
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