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UC2288
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
UC2288图片
CAS NO:1394011-91-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1 g电议

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 activep21attenuator (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 andRafkinases even at 10 μM[1].

体外研究
(In Vitro)

UC2288 (0-10 μM; 24 hours) decreases p21 protein level, but has no effects on other proteins[1].
UC2288 (0-10 μM; 24 hours) decreases p21 mRNA expression transcriptionally or post-transcriptionally but independently of p53[1].

Western Blot Analysis[1]

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[1]

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[2].
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[3].

Animal Model:Eight-week old, athymic nude (NCr nu/nu) mice injected subcutaneously with HCT116 and ACHN cancer cells(2.5x106)[2]
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[3]
Dosage:10 mg/kg
Administration:Intraperitoneal injection; 4 times in 7 days
Result:Ameliorated MPTP induced PD progression through inhibition of neuroinammation.
分子量

481.82

性状

Solid

Formula

C20H18ClF6N3O2

CAS 号

1394011-91-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
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 mg5 mg10 mg
1 mM2.0755 mL10.3773 mL20.7546 mL
5 mM0.4151 mL2.0755 mL4.1509 mL
10 mM0.2075 mL1.0377 mL2.0755 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。

*以上所有助溶剂都可在本网站选购。