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.
For research use only. We do not sell to patients.
- Purity : 98.05%
- CAS No.: 2050524-24-6
- Formula: C17H12ClN5O2S
- Molecular Weight:385.83
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PI3Kδ 1 nM (IC50) |
PI3Kα 51 nM (IC50) |
PI3Kβ 29 nM (IC50) |
PI3Kγ 37 nM (IC50) |
Cellular Effect
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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] |
In Vitro
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. Further protocols information, click here.
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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).
In Vivo
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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CAS No. 2050524-24-6
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Appearance Solid
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Molecular Weight 385.83
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
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)
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.
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.
In Vivo Dissolution Calculator
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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
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BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
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Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
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, 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 |
FD223 Related Classifications
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