1-(4-氯-3-(三氟甲基)苯基)-3-((1r，4r)-4-(5-(三氟甲基)吡啶-2-基氧基)环己基)脲|UC2288|cas:1394011-91-6|西域试剂

1-(4-氯-3-(三氟甲基)苯基)-3-((1r，4r)-4-(5-(三氟甲基)吡啶-2-基氧基)环己基)脲,UC2288,99.92%

产品编号：Bellancom-112780| CAS NO：1394011-91-6| 分子式：C₂₀H₁₈ClF₆N₃O₂| 分子量：481.82

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货号	价格	库存与货期
Bellancom-112780	￥1700.00	杭州北京（现货）
Bellancom-112780	￥2560.00	杭州北京（现货）
Bellancom-112780	￥4865.00	杭州北京（现货）
Bellancom-112780	￥7300.00	杭州北京（现货）
Bellancom-112780	￥9230.00	杭州北京（现货）

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1-(4-氯-3-(三氟甲基)苯基)-3-((1r，4r)-4-(5-(三氟甲基)吡啶-2-基氧基)环己基)脲

产品介绍

UC2288 是一种新型的、具有细胞通透性和口服活性的 p21 衰减试剂 (对 p21 具有相对选择性活性)，基于索拉非尼 (HY-10201) 的结构合成。UC2288 在不依赖 p53 的情况下下调 p21 mRNA 的表达，降低 p21 蛋白水平，对 p21 蛋白的稳定性影响很小。UC2288 对VEGFR2 和 Raf 激酶没有抑制作用，即使在 10 μM。

生物活性

UC2288 is a novel, cell-permeable, and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 decreases p21 mRNA expression independently of p53, and attenuates p21 protein levels with minimal effect on p21 protein stability. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM.

体外研究

UC2288 (0-10 μM; 24 hours) decreases p21 protein level, but has no effects on other proteins.
UC2288 (0-10 μM; 24 hours) decreases p21 mRNA expression transcriptionally or post-transcriptionally but independently of p53.

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

Western Blot Analysis

Cell Line:	HK2 (normal kidney), 786-O (RCC), Caki-1 (RCC), ACHN (RCC) and HEY (ovarian cancer) cells
Concentration:	0 μM; 1 μM; 3 μM; 10 μM
Incubation Time:	24 hours
Result:	Decreased p21 protein expression.

RT-PCR

Cell Line:	p53-mutant RCC cell line 786-O
Concentration:	10 μM
Incubation Time:	24 hours
Result:	Decreased p21 mRNA independent of p53 expression.

体内研究
(In Vivo)

UC2888 (oral gavage; 15 mg/kg; 3 times a week; 4 weeks) co-treatment with imetelstat significantly suppresses tumor growth and does not effect mice weight.
UC2288 (intraperitoneal injection; 10 mg/kg; 4 times in 7 days) attenuates MPTP-induced behavioral impairment, prevents activation of MAPK pathway in the MPTP-treated mice brain. MPTP treatment raises TNF-α, IL-6 and IL-1β levels in MPTP treated mice brain, but UC2288 signicantly decreases MPTP-induced TNF-α, IL-6 levels, but IL-1β is not decreased in brain.

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

Animal Model:	Eight-week old, athymic nude (NCr nu/nu) mice injected subcutaneously with HCT116 and ACHN cancer cells(2.5x10⁶)
Dosage:	15 mg/kg
Administration:	Oral gavage; 3 times a week; 4 weeks; co-treatment with imetelstat
Result:	Combined treatment with imetelstat synergistically inhibited tumor growth in mice.

Animal Model:	MPTP-induced C57BL6 Parkinson’s disease mice model
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; 4 times in 7 days
Result:	Ameliorated MPTP induced PD progression through inhibition of neuroinammation.

体内研究

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

Animal Model:	Eight-week old, athymic nude (NCr nu/nu) mice injected subcutaneously with HCT116 and ACHN cancer cells(2.5x10⁶)
Dosage:	15 mg/kg
Administration:	Oral gavage; 3 times a week; 4 weeks; co-treatment with imetelstat
Result:	Combined treatment with imetelstat synergistically inhibited tumor growth in mice.

Animal Model:	MPTP-induced C57BL6 Parkinson’s disease mice model
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; 4 times in 7 days
Result:	Ameliorated MPTP induced PD progression through inhibition of neuroinammation.

体内研究

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

Animal Model:	Eight-week old, athymic nude (NCr nu/nu) mice injected subcutaneously with HCT116 and ACHN cancer cells(2.5x10⁶)
Dosage:	15 mg/kg
Administration:	Oral gavage; 3 times a week; 4 weeks; co-treatment with imetelstat
Result:	Combined treatment with imetelstat synergistically inhibited tumor growth in mice.

Animal Model:	MPTP-induced C57BL6 Parkinson’s disease mice model
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; 4 times in 7 days
Result:	Ameliorated MPTP induced PD progression through inhibition of neuroinammation.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (103.77 mM; Need ultrasonic)

Ethanol : 12.5 mg/mL (25.94 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0755 mL	10.3773 mL	20.7546 mL
5 mM	0.4151 mL	2.0755 mL	4.1509 mL
10 mM	0.2075 mL	1.0377 mL	2.0755 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 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.32 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.32 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。