FPFT-2216|cas:2367619-87-0|西域试剂

FPFT-2216,99.35%

产品编号：Bellancom-145319| CAS NO：2367619-87-0| 分子式：C₁₂H₁₂N₄O₃S| 分子量：292.31

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-145319	￥3000.00	杭州北京（现货）
Bellancom-145319	￥4500.00	杭州北京（现货）
Bellancom-145319	￥9500.00	杭州北京（现货）

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FPFT-2216

产品介绍

FPFT-2216 是一种“分子胶水”化合物，可降解磷酸二酯酶 6D (PDE6D)、锌指转录因子 Ikaros (IKZF1)、Aiolos (IKZF3) 和酪蛋白激酶 1α (CK1α)。FPFT-2216 可用于癌症和炎症疾病的研究。

生物活性

FPFT-2216, a “molecular glue” compound, degrades phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3), and casein kinase 1α (CK1α). FPFT-2216 can be used for the research of cancer and inflammatory disease.

体外研究

FPFT-2216 (1 μM; 5 hours) is able to degrade PDE6D, in addition to its known targets IKZF1, IKZF3, and CK1α in MOLT4 cells.
FPFT-2216 (1 μM; 0 h, 2 h, 4 h, 6 h, 16 h, 24 h) shows complete degradation of PDE6D within 2 h, and the degradation of PDE6D persists for at least 24 h in MOLT4 cells.
FPFT-2216 (0 nM, 1.6 nM, 8 nM, 40 nM, 200 nM, 1 μM; 4 h) exhibits over 50% degradation of PDE6D at a dose of 8 nM, while maximum degradation of PDE6D along with IKZF1, IKZF3, and CK1α at a dose of 200 nM in MOLT4 cells.
FPFT-2216 does not impede the growth of KRAS^G12C-dependent MIA PaCa-2 cells.
FPFT-2216 (10, 20, 40 µM; 14 or 24 h) highly up-regulates the production of IL-2 although it is less potent than that of Pomalidomide in Naive CD4⁺ T cells.
FPFT-2216 (10 µM; 14 or 24 h) degrades IKZF1 and CK-1α among ubiquitin–proteasomal degradative substrates of immunomodulatory drugs (IMiDs) in Naive CD4⁺ T cells.

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

Western Blot Analysis

Cell Line:	MOLT4 cells
Concentration:	1 μM
Incubation Time:	0 h, 2 h, 4 h, 6 h, 16 h, 24 h
Result:	Showed complete degradation of PDE6D within 2 h, and the degradation of PDE6D persisted for at least 24 h.

Western Blot Analysis

Cell Line:	MOLT4 cells
Concentration:	0 nM, 1.6 nM, 8 nM, 40 nM, 200 nM, 1 μM
Incubation Time:	4 h
Result:	Exhibited over 50% degradation of PDE6D at a dose of 8 nM, while maximum degradation of PDE6D along with IKZF1, IKZF3, and CK1α at a dose of 200 nM.

体内研究
(In Vivo)

FPFT-2216 (30 mg/kg; p.o. or i.p.) induces significant degradation of CK-1α, and IKZF1 in CRBN^I391V mice.

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

Animal Model:	CRBN^I391V mice
Dosage:	30 mg/kg (solubilized in 0.5% carboxymethylcellulose/sodium and 0.25% Tween 80)
Administration:	p.o. or i.p.
Result:	Induced significant degradation of CK-1α, and IKZF1.

体内研究

FPFT-2216 (30 mg/kg; p.o. or i.p.) induces significant degradation of CK-1α, and IKZF1 in CRBN^I391V mice.

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

Animal Model:	CRBN^I391V mice
Dosage:	30 mg/kg (solubilized in 0.5% carboxymethylcellulose/sodium and 0.25% Tween 80)
Administration:	p.o. or i.p.
Result:	Induced significant degradation of CK-1α, and IKZF1.

体内研究

FPFT-2216 (30 mg/kg; p.o. or i.p.) induces significant degradation of CK-1α, and IKZF1 in CRBN^I391V mice.

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

Animal Model:	CRBN^I391V mice
Dosage:	30 mg/kg (solubilized in 0.5% carboxymethylcellulose/sodium and 0.25% Tween 80)
Administration:	p.o. or i.p.
Result:	Induced significant degradation of CK-1α, and IKZF1.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (342.10 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.4210 mL	17.1051 mL	34.2103 mL
5 mM	0.6842 mL	3.4210 mL	6.8421 mL
10 mM	0.3421 mL	1.7105 mL	3.4210 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 (8.55 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.55 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 (8.55 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.55 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 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: 2.5 mg/mL (8.55 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (8.55 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玉米油中，混合均匀。