Molecular Formula | C19H17NO5S |
Molar Mass | 371.41 |
Density | 1.423±0.06 g/cm3(Predicted) |
Boling Point | 538.0±50.0 °C(Predicted) |
Solubility | DMSO : 30 mg/mL (80.77 mM) |
pKa | 0.55±0.20(Predicted) |
Storage Condition | -20°C |
In vitro study | SF2523 prevents BRD4 from binding to the MYCN promoter PS1/PS2, inhibits M1-M2 transition, and reduces p-Akt and N-MYC levels in several neuroblastoma cell lines. Treatment of SF2523 reduced the protein levels of MYCN and Cyclin D1; Through the phosphorylation of tissue AKT in Ser473, the activation of AKT was inhibited. SF2523 strongly interacted with full-length BRD4 (Kd = 140 nM) and had similar affinity to BD1 of BRD4 (Kd = 150 nM); but its affinity for BD2 of BRD4 is weak (Kd = 710 nM). Comparing the binding affinity of SF2523 to the BDs of other proteins, it was found that it was similar to the BDs binding affinity of BRD4, BRD2 and BRD3, while it had intermediate binding affinity to the BDs of CECR2 and BRDT, but the binding affinity for other BDs is much weaker. |
In vivo study | SF2523 inhibits spontaneous metastasis and tumor growth. SF2523 is active in animal models and has been found to have no toxic effects in Orthotopic Pancreatic cancer models, multiple myeloma models, renal cell carcinoma models, neuroblastoma xenograft models. SF2523 targets PI3K and BRD4 driven oncogenic pathways in vivo. Compared to other equivalent PI3K inhibition and BRD4 inhibitor combinations, SF2523 has less toxic effects on the host. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.692 ml | 13.462 ml | 26.925 ml |
5 mM | 0.538 ml | 2.692 ml | 5.385 ml |
10 mM | 0.269 ml | 1.346 ml | 2.692 ml |
5 mM | 0.054 ml | 0.269 ml | 0.538 ml |
biological activity | SF2523 is a potent, highly selective PI3K inhibitor for PI3Kα, PI3Kγ, DNA-PK, the IC50 values of BRD4 and mTOR were 34 nM, 158 nM, 9 nM, 241 nM and 280 nM, respectively. |
Target | Value |
DNA-PK (Cell-free assay) | 9 nM |
PI3Kα (Cell-free assay) | 34 nM |
PI3Kγ (Cell-free assay) | 158 nM |
BRD4 (Cell-free assay) | 241 nM |
mTOR (Cell-free assay) | 280 nM |