FD223|cas:2050524-24-6|西域试剂

FD223,98.68%

产品编号：Bellancom-132231| CAS NO：2050524-24-6| 分子式：C₁₇H₁₂ClN₅O₂S| 分子量：385.83

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-132231	￥3000.00	杭州北京（现货）
Bellancom-132231	￥4800.00	杭州北京（现货）
Bellancom-132231	￥9500.00	杭州北京（现货）
Bellancom-132231	￥14500.00	杭州北京（现货）

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FD223

产品介绍

FD223 是一种有效且选择性的磷酸肌醇3-激酶δ (PI3Kδ) 抑制剂。FD223 显示出高效价 (IC₅₀=1 nM) 和对其他异构体的良好选择性 (α、β 和 γ 的IC₅₀ 值分别为 51 nM、29 nM 和 37nM）。FD223通过抑制 p-AKT Ser473 有效抑制急性髓系白血病 (AML) 细胞系的增殖，从而导致细胞周期 G1 期阻滞。FD223 在 AML 等白血病的研究中具有潜力。

生物活性

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.

体外研究

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.
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.
FD223 (MOLM-16 cells; 24 hours; 1-5 μM) arrests the cell cycle at the G1 phase similar to that of positive control Idelalisib.
FD223 (1-5 μM; 48 hours) dose-dependently induces cellular apoptosis.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis

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

Cell Line:	MOLM-16 cells
Concentration:	0.1-5 μM
Incubation Time:	16 hours
Result:	Dose-dependently reduced phosphorylation of Akt (Ser473).

体内研究
(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.
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%).

西域 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
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

体内研究

西域 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
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

体内研究

西域 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
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

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (259.18 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.48 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.48 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (6.48 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.48 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明