Home PI3K/Akt/mTOR PI3K inhibitor - DNA-PK inhibitor - Epigenetic Reader Domain inhibitor - mTOR inhibitor SF2523 For research use only.

SF2523

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.

SF2523 Chemical Structure

SF2523 Chemical Structure

CAS No. 1174428-47-7

Purity & Quality Control

Batch: S858901 DMSO]29 mg/mL]false]Ethanol]7 mg/mL]false]Water]Insoluble]false Purity: 99.04%
99.04

SF2523 Related Products

Signaling Pathway

PI3K Signaling Pathways

PI3K Signaling Pathway

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.
Targets
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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models Nude mice (8-wk old, female, NSG) with xenografted tumor
Dosages 50 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 371.41 Formula

C19H17NO5S
CAS No. 1174428-47-7 SDF Download SF2523 SDF
Smiles C1COCCN1C2=CC(=O)C3=C(O2)C(=CS3)C4=CC5=C(C=C4)OCCO5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 29 mg/mL ( (78.08 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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