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SF2523

Catalog No. T3986   CAS 1174428-47-7

SF2523 is a highly selective and potent inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
SF2523, CAS 1174428-47-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 54.00
5 mg In stock $ 135.00
10 mg In stock $ 234.00
25 mg In stock $ 460.00
1 mL * 10 mM (in DMSO) In stock $ 117.00
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Purity: 98.06%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SF2523 is a highly selective and potent inhibitor.
Targets&IC50 mTOR:280 nM, PI3Kγ:158 nM, BRD4:241 nM, PI3Kα:34 nM, DNA-PK:9 nM
In vitro 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].
In vivo 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].
Molecular Weight 371.41
Formula C19H17NO5S
CAS No. 1174428-47-7

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 30 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Andrews FH, et al. Dual-activity PI3K-BRD4 inhibitor for the orthogonal inhibition of MYC to block tumor growth and metastasis. Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):E1072-E1080.

Related compound libraries

This product is contained In the following compound libraries:
Stem Cell Differentiation Compound Library Anti-Obesity Compound Library Kinase Inhibitor Library Histone Modification Compound Library Pyroptosis Compound Library Anti-Liver Cancer Compound Library HIF-1 Signaling Pathway Compound Library PPI Inhibitor Library PI3K-AKT-mTOR Compound Library Glycolysis Compound Library

Related Products

Related compounds with same targets
DMNB AZD-7648 OSI-027 SF2523 ETP-45658 PIK-75 hydrochloride PI-3065 PI3K-IN-1

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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.

Keywords

SF2523 1174428-47-7 Chromatin/Epigenetic DNA Damage/DNA Repair PI3K/Akt/mTOR signaling DNA-PK Epigenetic Reader Domain PI3K mTOR SF 2523 Inhibitor SF-2523 Phosphoinositide 3-kinase DNA-dependent protein kinase inhibit inhibitor