SF2523
Based on 2 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.34%
- No. CAS: 1174428-47-7
- Fòrmula: C19H17NO5S
- Peso molecular:371.41
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SF2523
More
Actividad biológica
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PI3Kα 34 nM (IC50) |
PI3Kγ 158 nM (IC50) |
BRD4 (BD1) 241 nM (IC50) |
DNA-PK 9 nM (IC50) |
mTOR 280 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 786-0 | IC50 |
3.3 μM
Compound: 43
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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
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[PMID: 23410005] |
| BT-474 | IC50 |
3.8 μM
Compound: 43
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Inhibition of human BT474 cell proliferation after 72 hrs by spectrophotometric analysis
Inhibition of human BT474 cell proliferation after 72 hrs by spectrophotometric analysis
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[PMID: 23410005] |
| NCI-H1299 | IC50 |
0.9 μM
Compound: 43
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Inhibition of human H1299 cell proliferation after 72 hrs by spectrophotometric analysis
Inhibition of human H1299 cell proliferation after 72 hrs by spectrophotometric analysis
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[PMID: 23410005] |
| PC-3 | IC50 |
1.6 μM
Compound: 43
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Inhibition of human PC3 cell proliferation after 72 hrs by spectrophotometric analysis
Inhibition of human PC3 cell proliferation after 72 hrs by spectrophotometric analysis
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[PMID: 23410005] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1174428-47-7
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Appearance Solid
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Peso molecular 371.41
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Fòrmula C19H17NO5S
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Color Light yellow to khaki
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SMILES
O=C1C=C(N2CCOCC2)OC3=C1SC=C3C4=CC=C(OCCO5)C5=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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J Control Release
2023 Feb:354:80-90. PMID: 36599397 -
Sci Rep
QSAR analysis on a large and diverse set of potent phosphoinositide 3-kinase gamma (PI3Kγ) inhibitors using MLR and ANN methods. [Abstract]2022 Apr 12;12(1):6090. PMID: 35414065
Solvente y solubilidad
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Carlino L, et al. Dual Kinase-Bromodomain Inhibitors in Anticancer Drug Discovery: A Structural andPharmacological Perspective. J Med Chem. 2016 Oct 27;59(20):9305-9320. [Content Brief]
[2]. 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. [Content Brief]
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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