FD223

Name: FD223
Brand: MedChemExpress
SKU: HY-132231
Rating: 4.5 (1 reviews)

Cat. No.: HY-132231 Purity: 98.05%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

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

FD223 Chemical Structure

CAS No. : 2050524-24-6

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 231	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 231	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 210	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 340	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 680	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1100	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1800	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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View All PI3K Isoform Specific Products:

View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

PI3Kδ

1 nM (IC₅₀)

PI3Kα

51 nM (IC₅₀)

PI3Kβ

29 nM (IC₅₀)

PI3Kγ

37 nM (IC₅₀)

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

Molecular Weight

385.83

Formula

C₁₇H₁₂ClN₅O₂S

CAS No.

2050524-24-6

Appearance

Solid

Color

Off-white to brown

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

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.
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 (6.48 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:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 98.05%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (249 KB) LCMS (106 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

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:

FD2232050524-24-6FD 223FD-223PI3KApoptosisPhosphoinositide 3-kinaseselectivetumorgrowthBALB/cnudemiceMOLM-16AMLInhibitorinhibitorinhibit

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FD223

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Complete Stock Solution Preparation Table

FD223 Related Classifications

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