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SF2523

Catalog No. T3986   CAS 1174428-47-7

SF2523 is a highly selective and potent inhibitor.

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SF2523 Chemical Structure
SF2523, CAS 1174428-47-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 31.00
5 mg In stock $ 72.00
10 mg In stock $ 122.00
25 mg In stock $ 289.00
50 mg In stock $ 455.00
100 mg In stock $ 672.00
500 mg In stock $ 1,430.00
1 mL * 10 mM (in DMSO) In stock $ 79.00
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Purity: 98.06%
Purity: 97.78%
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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 Treatment with SF2523 leads to a reduction in the protein levels of MYCN and Cyclin D1, targets of MYCN. It also impedes AKT activation by preventing the phosphorylation at Ser473 and results in the removal of BRD4 from MYCN promoter sites. SF2523 exhibits a strong interaction with full-length BRD4 (Kd=140 nM), showing a similar affinity for BRD4's first bromodomain (BD1) (Kd=150 nM) but a weaker affinity for its second bromodomain (BD2) (Kd=710 nM). When comparing the binding affinities of SF2523 to bromodomains (BDs) of different proteins, it demonstrates equal binding to BDs of BRD4, BRD2, and BRD3; a moderate binding to BDs of CECR2 and BRDT; and significantly weaker binding to other BDs[1].
In vivo Treatment with SF2523 significantly reduces tumor volume without causing gross toxicity in mice, as evidenced by stable body weight. Furthermore, tumors in mice treated with SF2523 exhibit notably lower levels of MYCN, pAKT, and Cyclin D1 compared to those in mice treated with the vehicle[1].
Molecular Weight 371.41
Formula C19H17NO5S
CAS No. 1174428-47-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (26.92 mM)

TargetMolReferences 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:
Anti-Cancer Active Compound Library Inhibitor Library Kinase Inhibitor Library Neuronal Differentiation Compound Library Epigenetics Compound Library Anti-Obesity Compound Library Chromatin Modification Compound Library Cancer Cell Differentiation Compound Library Neural Regeneration Compound Library Oxidation-Reduction Compound Library

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Keywords

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

 

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