1. PI3K/Akt/mTOR
    Apoptosis
  2. PI3K
    Apoptosis
  3. FD223

FD223 

Cat. No.: HY-132231
Handling Instructions

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

FD223 Chemical Structure

CAS No. : 2050524-24-6

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Description

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[1].

IC50 & Target[1]

PI3Kδ

1 nM (IC50)

PI3Kα

51 nM (IC50)

PI3Kβ

29 nM (IC50)

PI3Kγ

37 nM (IC50)

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].

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 (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].

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.
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Storage

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FD223
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