化合物SF2523 T3986

Product Introduction
Bioactivity


英文名: SF2523

描述: SF2523 是一种选择性PI3K 抑制剂，抑制DNA-PK、PI3Kα、PI3Kγ、BRD4 和 mTOR，IC50分别为 9 nM、34 nM、158 nM、241 nM 和 280 nM。

体外活性: SF2523 treatment decreases protein levels of MYCN and Cyclin D1, the MYCN target. SF2523 treatment inhibits AKT activation by blocking phosphorylation of AKT at Ser473. SF2523 treatment leads to the displacement of BRD4 from both MYCN promoter sites. SF2523 interacts robustly with the full-length BRD4 (Kd=140 nM) and exhibits comparable affinity to the BRD4 first BD (BD1) (Kd=150 nM), however it binds more weakly to the second BD (BD2) of BRD4 (Kd=710 nM). Comparison of binding affinities of SF2523 for BDs of other proteins reveal that it binds equally well to BDs of BRD4, BRD2, and BRD3; shows moderate binding to BDs of CECR2 and BRDT; but associates much weaker with other BDs[1].

体内活性: SF2523 treatment results in a significant reduction of tumor volume compared with control. Importantly, SF2523 shows no gross toxicity to the treated mice, because there is no notable change in body weight. Tumors from SF2523-treated mice have significantly reduced MYCN, pAKT, and Cyclin D1 levels compared with levels of these proteins in vehicle-treated mice tumors[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 10 mg/mL (26.92 mM)


关键字: SF 2523 | SF-2523 | Inhibitor | PI3K | Phosphoinositide 3-kinase | Epigenetic Reader Domain | DNA-dependent protein kinase | DNA-PK | inhibit | SF2523

相关产品: ETP-45658 | OSI-027 | KU-57788 | Pictilisib dimethanesulfonate | Samotolisib | DMNB | Leniolisib | (R)-(-)-Rolipram | ETP-46464 | LY294002

相关库: Pyroptosis Compound Library | Glutamine Metabolism Compound Library | Angiogenesis related Compound Library | Inhibitor Library | Kinase Inhibitor Library | Epigenetics Compound Library | Anti-Cancer Active Compound Library | DNA Damage & Repair Compound Library | PPI Inhibitor Library | Reprogramming Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途