2. PI3K/Akt/mTOR Epigenetics Cell Cycle/DNA Damage
  3. PI3K Epigenetic Reader Domain DNA-PK
  4. SF2523

SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.

For research use only. We do not sell to patients.

SF2523 Chemical Structure

SF2523 Chemical Structure

CAS No. : 1174428-47-7

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10 mM * 1 mL in DMSO
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Customer Review

Based on 2 publication(s) in Google Scholar

SF2523 Related Antibodies

Top Publications Citing Use of Products

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.

IC50 & Target[1]

PI3Kα

34 nM (IC50)

PI3Kγ

158 nM (IC50)

BRD4 (BD1)

241 nM (IC50)

DNA-PK

9 nM (IC50)

mTOR

280 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
786-0 IC50
3.3 μM
Compound: 43
Inhibition of human 786-O cell proliferation after 72 hrs by spectrophotometric analysis
Inhibition of human 786-O cell proliferation after 72 hrs by spectrophotometric analysis
[PMID: 23410005]
BT-474 IC50
3.8 μM
Compound: 43
Inhibition of human BT474 cell proliferation after 72 hrs by spectrophotometric analysis
Inhibition of human BT474 cell proliferation after 72 hrs by spectrophotometric analysis
[PMID: 23410005]
NCI-H1299 IC50
0.9 μM
Compound: 43
Inhibition of human H1299 cell proliferation after 72 hrs by spectrophotometric analysis
Inhibition of human H1299 cell proliferation after 72 hrs by spectrophotometric analysis
[PMID: 23410005]
PC-3 IC50
1.6 μM
Compound: 43
Inhibition of human PC3 cell proliferation after 72 hrs by spectrophotometric analysis
Inhibition of human PC3 cell proliferation after 72 hrs by spectrophotometric analysis
[PMID: 23410005]
In Vitro

SF2523 treatment decreases protein levels of MYCN and Cyclin D1, the MYCN target, and 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[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SF2523 Related Antibodies
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, as there is no notable change in body weight. Tumors from SF2523-treated mice have markedly reduced MYCN, pAKT, and Cyclin D1 levels compared with levels of these proteins in vehicle-treated mice tumors[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

371.41

Formula

C19H17NO5S
CAS No.
Appearance

Solid

Color

Light yellow to khaki

SMILES

O=C1C=C(N2CCOCC2)OC3=C1SC=C3C4=CC=C(OCCO5)C5=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (80.77 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6924 mL 13.4622 mL 26.9244 mL
5 mM 0.5385 mL 2.6924 mL 5.3849 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Animal Administration
[2]

Mice: After 20 d of tumor implantation, mice are treated with either (i) 30 mg/kg of SF2523 formulated in 15% DMA+30% captisol, (ii) 30 mg/kg of JQ1 formulated in 30% captisol in combination with 30 mg/kg of BKM120 formulated in 15% ethanol+15% cremaphore, (iii) vehicle (15% ethanol+15% cremaphore, as control), or (iv) another vehicle (15% DMA+30% captisol, as control) five times a week, until tumors are removed on day 35[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6924 mL 13.4622 mL 26.9244 mL 67.3111 mL
5 mM 0.5385 mL 2.6924 mL 5.3849 mL 13.4622 mL
10 mM 0.2692 mL 1.3462 mL 2.6924 mL 6.7311 mL
15 mM 0.1795 mL 0.8975 mL 1.7950 mL 4.4874 mL
20 mM 0.1346 mL 0.6731 mL 1.3462 mL 3.3656 mL
25 mM 0.1077 mL 0.5385 mL 1.0770 mL 2.6924 mL
30 mM 0.0897 mL 0.4487 mL 0.8975 mL 2.2437 mL
40 mM 0.0673 mL 0.3366 mL 0.6731 mL 1.6828 mL
50 mM 0.0538 mL 0.2692 mL 0.5385 mL 1.3462 mL
60 mM 0.0449 mL 0.2244 mL 0.4487 mL 1.1219 mL
80 mM 0.0337 mL 0.1683 mL 0.3366 mL 0.8414 mL
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SF2523 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SF25231174428-47-7SF 2523SF-2523PI3KEpigenetic Reader DomainDNA-PKPhosphoinositide 3-kinaseDNA-dependent protein kinaseInhibitorinhibitorinhibit

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