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FD223

产品编号 T35531 CAS 2050524-24-6

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].

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FD223, CAS 2050524-24-6

规格	价格/CNY	货期
2 mg	￥ 1,540	5日内发货
5 mg	￥ 2,610	5日内发货
25 mg	￥ 9,160	6-8周
50 mg	￥ 11,900	6-8周
100 mg	￥ 17,500	6-8周
1 mL * 10 mM (in DMSO)	￥ 2,730	5日内发货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	FD223 is a potent, selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor with a marked affinity (IC50=1 nM), demonstrating notable selectivity against other isoforms (IC50s: α=51 nM, β=29 nM, γ=37 nM). This compound effectively suppresses the proliferation of acute myeloid leukemia (AML) cell lines by inhibiting p-AKT Ser473, thereby inducing G1 phase cell cycle arrest. FD223 holds promise for leukemia research, particularly in AML[1].
靶点活性	PI3Kγ:37 nM (IC50), PI3Kα:51 nM (IC50), PI3Kβ:29 nM (IC50), PI3Kδ:1 nM (IC50)
体外活性	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].
体内活性	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].

分子量	385.83
分子式	C17H12ClN5O2S
CAS No.	2050524-24-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 100 mg/mL (259.18 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	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
	20 mM	0.1296 mL	0.648 mL	1.2959 mL	3.2398 mL
	50 mM	0.0518 mL	0.2592 mL	0.5184 mL	1.2959 mL
	100 mM	0.0259 mL	0.1296 mL	0.2592 mL	0.648 mL

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参考文献

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.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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