UC2288
目录号: PL07018 纯度: ≥99%
CAS No. :1394011-91-6
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中文名称
UC2288
英文名称
UC2288
英文别名
UC2288;UC 2288, trans;BDBM158490;UC 2288;US9029401, 2288;Z1993522716;1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(trans-4-((5-(trifluoromethyl)pyridin-2-yl)oxy)cyclohexyl)urea;1-[4-chloro-3-(trifluoromethyl)phenyl]-3-(4-{[5-(trifluoromethyl)pyridin-2-yl]oxy}cyclohexyl)urea;1-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1r,4r)-4-{[5-(trifluoromethyl)pyridin-2-yl]oxy}cyclohexyl]urea;1
Cas No.
1394011-91-6
分子式
C20H18ClF6N3O2
分子量
481.82
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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.
性状
Solid
体外研究(In Vitro)
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.
has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
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.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Hiromi I Wettersten, et al. A Novel p21 Attenuator Which Is Structurally Related to Sorafenib. Cancer Biol Ther. 2013 Mar;14(3):278-85.
[2]. Romi Gupta, et al. Synergistic tumor suppression by combined inhibition of telomerase and CDKN1A. Proc Natl Acad Sci U S A. 2014 Jul 29;111(30):E3062-71.
溶解度数据
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
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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