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SF2523 PI3K inhibitor

Name: SF2523
Brand: Selleck Chemicals
SKU: S8589
Rating: 5 (3 reviews)

Cat.No.S8589

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.

Chemical Structure

Molecular Weight: 371.41

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.04

Related Targets	Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Other PI3K Inhibitors	GDC-0077 (Inavolisib) SAR405 Quercetin (Sophoretin) LY294002 XL147 analogue Tersolisib (STX-478) Buparlisib (BKM120) 740 Y-P (PDGFR 740Y-P) GO-203 TFA Eganelisib (IPI-549)

Chemical Information, Storage & Stability

Molecular Weight	371.41	Formula	C₁₉H₁₇NO₅S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1174428-47-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1COCCN1C2=CC(=O)C3=C(O2)C(=CS3)C4=CC5=C(C=C4)OCCO5

Solubility

In vitro
Batch:

DMSO : 29 mg/mL (78.08 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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
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. This compound treatment decreases protein levels of MYCN and Cyclin D1, the MYCN target, and inhibits AKT activation by blocking phosphorylation of AKT at Ser473. It 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 this chemical 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.
In vivo	SF2523 blocks spontaneous metastasis and tumour growth. This compound 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. It targets PI3K-driven and BRD4-driven oncogenic pathways in vivo. It is less toxic to the host organism in vivo than a combination of an equipotent PI3K inhibitor and BRD4 inhibitor.
References	[1] http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.6b00438 [2] http://cancerres.aacrjournals.org/content/76/14_Supplement/LB-211.short [3] https://pubmed.ncbi.nlm.nih.gov/28137841/

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