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。

SF2523 is a highly selective and potent inhibitor.

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].

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].

1174428-47-7

C19H17NO5S

371.41

DMSO:30 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years