UC2288

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

UC2288是一种相对选择性的p21衰减剂，是在索拉非尼的基础上合成的。 UC2288 降低 p21 蛋白水平，对 p21 蛋白稳定性影响极小。

UC2288 is a relatively selective p21 attenuator which is synthesized based Sorafenib. UC2288 attenuates p21 protein levels with minimal effect on p21 protein stability.(In Vitro):UC2288 (0-10 μM; 24 hours) decreases p21 mRNA expression transcriptionally or post-transcriptionally but independently of p53. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM.(In Vivo):UC2288 (10 mg/kg; i.p.) 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.UC2888 (15 mg/kg; oral) co-treatment with imetelstat significantly suppresses tumor growth and does not effect mice weight.

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.

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.

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Apoptosis

MDM2-p53

mGluR4

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1394011-91-6

481.82

C20H18ClF6N3O2

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (103.77 mM)

FC(F)(F)c1ccc(O[C@H]2CC[C@@H](CC2)NC(=O)Nc2ccc(Cl)c(c2)C(F)(F)F)nc1

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(-20℃)

With Ice Pack

≥ 2 years