For research use only.

Catalog No.S8589

1 publication

SF2523 Chemical Structure

CAS No. 1174428-47-7

SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.

Selleck's SF2523 has been cited by 1 publication

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Biological Activity

Description SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
DNA-PK [1]
(Cell-free assay)
PI3Kα [1]
(Cell-free assay)
PI3Kγ [1]
(Cell-free assay)
BRD4 [1]
(Cell-free assay)
mTOR [1]
(Cell-free assay)
9 nM 34 nM 158 nM 241 nM 280 nM
In vitro

SF2523 blocks BRD4 binding to MYCN promoter PS1/PS2. It blocks M1-M2 transition and decreases levels of p-AKT, N-MYC in several neuroblastoma cell lines. SF2523 treatment decreases protein levels of MYCN and Cyclin D1, the MYCN target, and inhibits AKT activation by blocking phosphorylation of AKT at Ser473[2]. 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 reveals 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[3].

In vivo SF2523 blocks spontaneous metastasis and tumor growth. SF2523 has demonstrated animal efficacy results without toxicity in the following 4 animal models: orthotopic pancreatic model, multiple myeloma model, renal cell carcinoma model, neuroblastoma xenograft model[2]. SF2523 targets PI3K-driven and BRD4-driven oncogenic pathways in vivo. SF2523 is less toxic to the host organism in vivo than a combination of an equipotent PI3K inhibitor and BRD4 inhibitor[3].


Cell Research:


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  • Cell lines: neuroblastoma SKNBE2 cell line
  • Concentrations: 5 μM
  • Incubation Time: 24 h
  • Method:

    SKNBE2 cells are serum-starved for 4 h, stimulated with 50 ng/mL IGF, and treated with 1 μM JQ1, 5 μM SF2523, 10 μM SF1126, 1 μM BKM120, 1 μM BEZ235, or 200 nM CAL101 for 24 h. Then, cells are harvested and total RNA is extracted; Perform RT-PCR.

    (Only for Reference)
Animal Research:


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  • Animal Models: Nude mice (8-wk old, female, NSG) with xenografted tumor
  • Dosages: 50 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 29 mg/mL (78.08 mM)
Ethanol 7 mg/mL (18.84 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 371.41


CAS No. 1174428-47-7
Storage powder
in solvent
Synonyms N/A
Smiles C1COCCN1C2=CC(=O)C3=C(O2)C(=CS3)C4=CC5=C(C=C4)OCCO5

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID