FD223
Based on 1 Customer Validation
FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML.
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- Pureza: 98.05%
- No. CAS: 2050524-24-6
- Fòrmula: C17H12ClN5O2S
- Peso molecular:385.83
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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PI3Kδ 1 nM (IC50) |
PI3Kα 51 nM (IC50) |
PI3Kβ 29 nM (IC50) |
PI3Kγ 37 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| EOL1 | IC50 |
2.82 μM
Compound: 13; FC-223
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Antiproliferative activity against human EOL1 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
Antiproliferative activity against human EOL1 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
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[PMID: 34237636] |
| HL-60 | IC50 |
2.25 μM
Compound: 13; FC-223
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Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
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[PMID: 34237636] |
| KARPAS-422 | GI50 |
1.09 μM
Compound: B7
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Growth inhibition of human KARPAS422 cells by CCK8 assay
Growth inhibition of human KARPAS422 cells by CCK8 assay
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[PMID: 28835805] |
| KG-1 | IC50 |
5.82 μM
Compound: 13; FC-223
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Antiproliferative activity against human KG-1 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
Antiproliferative activity against human KG-1 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
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[PMID: 34237636] |
| MCF7 | GI50 |
7.4 μM
Compound: B7
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Growth inhibition of human MCF7 cells after 72 hrs by SRB assay
Growth inhibition of human MCF7 cells after 72 hrs by SRB assay
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[PMID: 28835805] |
| MOLM-16 | IC50 |
0.87 μM
Compound: 13; FC-223
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Antiproliferative activity against human MOLM16 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
Antiproliferative activity against human MOLM16 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
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[PMID: 34237636] |
| NCI-H460 | GI50 |
7.61 μM
Compound: B7
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Growth inhibition of human NCI-H460 cells after 72 hrs by SRB assay
Growth inhibition of human NCI-H460 cells after 72 hrs by SRB assay
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[PMID: 28835805] |
| Pfeiffer | GI50 |
1.16 μM
Compound: B7
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Growth inhibition of human Pfeiffer cells by CCK8 assay
Growth inhibition of human Pfeiffer cells by CCK8 assay
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[PMID: 28835805] |
| T47D | GI50 |
4.4 μM
Compound: B7
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Growth inhibition of human T47D cells after 72 hrs by SRB assay
Growth inhibition of human T47D cells after 72 hrs by SRB assay
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[PMID: 28835805] |
| U-87MG ATCC | GI50 |
8.94 μM
Compound: B7
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Growth inhibition of human U87MG cells after 72 hrs by SRB assay
Growth inhibition of human U87MG cells after 72 hrs by SRB assay
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[PMID: 28835805] |
FD223 exhibits notable anti-proliferative activities in the p110δ-positive AML cell lines HL-60, MOLM-16, EOL-1 and KG-1, with the IC50 of 2.25 μM, 0.87 μM, 2.82 μM, and 5.82 μM, respectively. FD223 shows weak anti-proliferative activity against p110δ unexpressed MM.1R cell line, with the IC50 value of 23.13 μM[1].
FD223 (MOLM-16 cells; 0.1-5 μM; 16 hours) dose-dependently reduces phosphorylation of Akt (Ser473), which is consistent with the positive control Idelalisib, illustrating that the activity of PI3K/Akt pathway in MOLM-16 cell is blocked[1].
FD223 (MOLM-16 cells; 24 hours; 1-5 μM) arrests the cell cycle at the G1 phase similar to that of positive control Idelalisib[1].
FD223 (1-5 μM; 48 hours) dose-dependently induces cellular apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM-16 cells
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Concentration:1-5 μM
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Incubation Time:48 hours
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Result:Dose-dependently induced cellular apoptosis, which is superior to that of positive control Idelalisib.
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Cell Line:MOLM-16 cells
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Concentration:0.1-5 μM
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Incubation Time:16 hours
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Result:Dose-dependently reduced phosphorylation of Akt (Ser473).
FD223 (i.v.; dose of 2 mg/kg; p.o.; 10 mg/kg rats) shows a moderate plasma clearance rate after intravenous administration with C =0.191 L•h-1•kg-1. In the po route, it shows a half-life (t1/2) of 3.74 h and a Cmax of 1104 ng/mL, good oral plasma exposures (AUC0-∞>9000 h•ng/mL) and acceptable oral bioavailability (17.6%)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MOLM-16 xenograft model of BALB/c nude mice[1]
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Dosage:20 and 40 mg/kg
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Administration:P.o, per day for 14 consecutive days
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Result:Showed a dose-dependent tumor growth inhibition (TGI) of 31% for 20 mg/kg and 49% for 40 mg/kg
Chemical Information
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No. CAS 2050524-24-6
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Appearance Solid
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Peso molecular 385.83
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Fòrmula C17H12ClN5O2S
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Color Off-white to brown
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SMILES
O=S(C1=CC=CC=C1)(NC2=CC(C3=CN=C(NN=C4)C4=C3)=CN=C2Cl)=O
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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 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (259.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (6.48 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 (6.48 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5918 mL | 12.9591 mL | 25.9182 mL | 64.7954 mL |
| 5 mM | 0.5184 mL | 2.5918 mL | 5.1836 mL | 12.9591 mL | |
| 10 mM | 0.2592 mL | 1.2959 mL | 2.5918 mL | 6.4795 mL | |
| 15 mM | 0.1728 mL | 0.8639 mL | 1.7279 mL | 4.3197 mL | |
| 20 mM | 0.1296 mL | 0.6480 mL | 1.2959 mL | 3.2398 mL | |
| 25 mM | 0.1037 mL | 0.5184 mL | 1.0367 mL | 2.5918 mL | |
| 30 mM | 0.0864 mL | 0.4320 mL | 0.8639 mL | 2.1598 mL | |
| 40 mM | 0.0648 mL | 0.3240 mL | 0.6480 mL | 1.6199 mL | |
| 50 mM | 0.0518 mL | 0.2592 mL | 0.5184 mL | 1.2959 mL | |
| 60 mM | 0.0432 mL | 0.2160 mL | 0.4320 mL | 1.0799 mL | |
| 80 mM | 0.0324 mL | 0.1620 mL | 0.3240 mL | 0.8099 mL | |
| 100 mM | 0.0259 mL | 0.1296 mL | 0.2592 mL | 0.6480 mL |
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