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FD223

Catalog No.GC62973

FD223은 강력하고 선택적인 포스포이노시티드 3-키나제 델타(PI3Kδ) 억제제입니다. FD223은 높은 효능(IC50=1nM)과 다른 동형체(α, β 및 γ에 대해 각각 51nM, 29nM 및 37nM의 IC50)에 비해 우수한 선택성을 나타냅니다. FD223은 p-AKT Ser473을 억제하여 세포 주기 동안 G1기 정지를 유발함으로써 급성 골수성 백혈병(AML) 세포주의 증식을 효율적으로 억제합니다. FD223은 AML과 같은 백혈병 연구에 대한 잠재력이 있습니다.

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FD223 Chemical Structure

Cas No.: 2050524-24-6

Size 가격 재고 수량
5 mg
US$270.00
재고 있음
10 mg
US$432.00
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25 mg
US$855.00
재고 있음
50 mg
US$1,305.00
재고 있음

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents

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].

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].

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].

[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.

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Average Rating: 5 ★★★★★ (Based on Reviews and 19 reference(s) in Google Scholar.)

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