Cat. No.: HY-132231

FD223

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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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Pureté: 98.05%
CAS No.: 2050524-24-6
Formule: C₁₇H₁₂ClN₅O₂S
Masse moléculaire:385.83

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

FD223 Chemical Structure

CAS No.: 2050524-24-6

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

PI3Kδ

1 nM (IC₅₀)

PI3Kα

51 nM (IC₅₀)

PI3Kβ

29 nM (IC₅₀)

PI3Kγ

37 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform PI3K :

Cellular Effect

Cell Line	Type	Value	Description	References
EOL1	IC₅₀	2.82 μM Compound: 13; FC-223	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	[PMID: 34237636]
HL-60	IC₅₀	2.25 μM Compound: 13; FC-223	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	[PMID: 34237636]
KARPAS-422	GI₅₀	1.09 μM Compound: B7	Growth inhibition of human KARPAS422 cells by CCK8 assay Growth inhibition of human KARPAS422 cells by CCK8 assay	[PMID: 28835805]
KG-1	IC₅₀	5.82 μM Compound: 13; FC-223	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	[PMID: 34237636]
MCF7	GI₅₀	7.4 μM Compound: B7	Growth inhibition of human MCF7 cells after 72 hrs by SRB assay Growth inhibition of human MCF7 cells after 72 hrs by SRB assay	[PMID: 28835805]
MOLM-16	IC₅₀	0.87 μM Compound: 13; FC-223	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	[PMID: 34237636]
NCI-H460	GI₅₀	7.61 μM Compound: B7	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	[PMID: 28835805]
Pfeiffer	GI₅₀	1.16 μM Compound: B7	Growth inhibition of human Pfeiffer cells by CCK8 assay Growth inhibition of human Pfeiffer cells by CCK8 assay	[PMID: 28835805]
T47D	GI₅₀	4.4 μM Compound: B7	Growth inhibition of human T47D cells after 72 hrs by SRB assay Growth inhibition of human T47D cells after 72 hrs by SRB assay	[PMID: 28835805]
U-87MG ATCC	GI₅₀	8.94 μM Compound: B7	Growth inhibition of human U87MG cells after 72 hrs by SRB assay Growth inhibition of human U87MG cells after 72 hrs by SRB assay	[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.

Apoptosis Analysis^[1]

Cell Line:

MOLM-16 cells
Concentration:

1-5 μM
Incubation Time:

48 hours
Result:

Dose-dependently induced cellular apoptosis, which is superior to that of positive control Idelalisib.

Western Blot Analysis^[1]

Cell Line:

MOLM-16 cells
Concentration:

0.1-5 μM
Incubation Time:

16 hours
Result:

Dose-dependently reduced phosphorylation of Akt (Ser473).

In Vivo

FD223 (20 and 40 mg/kg; p.o, per day for 14 consecutive days) displays potent antitumor efficacy in MOLM-16 xenograft model with the tumor volume reduction of 49% at a dose of 40 mg/kg/day (po), and shows no significant toxicity in the preliminary safety assessment^[1].
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 (t_1/2) of 3.74 h and a Cmax of 1104 ng/mL, good oral plasma exposures (AUC_0-∞>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.

Animal Model:

MOLM-16 xenograft model of BALB/c nude mice^[1]
Dosage:

20 and 40 mg/kg
Administration:

P.o, per day for 14 consecutive days
Result:

Showed a dose-dependent tumor growth inhibition (TGI) of 31% for 20 mg/kg and 49% for 40 mg/kg

Chemical Information

CAS No. 2050524-24-6
Appearance Solid
Masse moléculaire 385.83
Formule C₁₇H₁₂ClN₅O₂S
Color Off-white to brown
SMILES

O=S(C1=CC=CC=C1)(NC2=CC(C3=CN=C(NN=C4)C4=C3)=CN=C2Cl)=O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5918 mL

12.9591 mL

25.9182 mL

5 mM

0.5184 mL

2.5918 mL

5.1836 mL

10 mM

0.2592 mL

1.2959 mL

2.5918 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 (6.48 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.

Protocol 2

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (251 KB)
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- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Yang C, et al. Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation [published online ahead of print, 2021 Jun 21]. Eur J Med Chem. 2021;223:113661. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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Voir tous les produits spécifiques à Isoform PI3K

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

FD223 Related Classifications

HY-132231 Related Classifications