Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SF2523 is a highly selective and potent inhibitor.
説明 | SF2523 is a highly selective and potent inhibitor. |
ターゲット&IC50 | mTOR:280 nM, PI3Kγ:158 nM, BRD4:241 nM, PI3Kα:34 nM, DNA-PK:9 nM |
In vitro | Treatment with SF2523 leads to a reduction in the protein levels of MYCN and Cyclin D1, targets of MYCN. It also impedes AKT activation by preventing the phosphorylation at Ser473 and results in the removal of BRD4 from MYCN promoter sites. SF2523 exhibits a strong interaction with full-length BRD4 (Kd=140 nM), showing a similar affinity for BRD4's first bromodomain (BD1) (Kd=150 nM) but a weaker affinity for its second bromodomain (BD2) (Kd=710 nM). When comparing the binding affinities of SF2523 to bromodomains (BDs) of different proteins, it demonstrates equal binding to BDs of BRD4, BRD2, and BRD3; a moderate binding to BDs of CECR2 and BRDT; and significantly weaker binding to other BDs[1]. |
In vivo | Treatment with SF2523 significantly reduces tumor volume without causing gross toxicity in mice, as evidenced by stable body weight. Furthermore, tumors in mice treated with SF2523 exhibit notably lower levels of MYCN, pAKT, and Cyclin D1 compared to those in mice treated with the vehicle[1]. |
分子量 | 371.41 |
分子式 | C19H17NO5S |
CAS No. | 1174428-47-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mg/mL (26.92 mM)
You can also refer to dose conversion for different animals. 詳細
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
SF2523 1174428-47-7 Chromatin/Epigenetic DNA Damage/DNA Repair PI3K/Akt/mTOR signaling DNA-PK Epigenetic Reader Domain PI3K mTOR SF 2523 SF-2523 Inhibitor Phosphoinositide 3-kinase DNA-dependent protein kinase inhibit inhibitor