| Identification | Back Directory | [Name]
UC2288 | [CAS]
1394011-91-6 | [Synonyms]
UC2288
1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(trans-4-((5-(trifluoromethyl)pyridin-2-yl)oxy)cyclohexyl)urea
Attenuator,786-O,Inhibitor,UC-2288,MDM-2/p53,inhibit,UC2288,ovarian,RCC,HK2,UC 2288,p21,sorafenib,p53-mutant,cancer | [Molecular Formula]
C20H18ClF6N3O2 | [MDL Number]
MFCD28139634 | [MOL File]
1394011-91-6.mol | [Molecular Weight]
481.82 |
| Chemical Properties | Back Directory | [Boiling point ]
491.9±45.0 °C(Predicted) | [density ]
1.45±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMF: 25 mg/ml; DMSO: 25 mg/ml; Ethanol: 25 mg/ml | [form ]
A solid | [pka]
12.88±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
UC2288 is a potent and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 potently inhibits cancer cell growth by inducing apoptosis. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM[1]. | [Biological Activity]
Cell permeable: yes | [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. |
| [References]
[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. DOI:10.4161/cbt.23374
[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. DOI:10.1073/pnas.1411370111
[3] Jun Hyung Im, et al. p21 inhibitor UC2288 ameliorates MPTP induced Parkinson’s disease progression through inhibition of oxidative stress and neuroinammation. Translational Medicine.Neurobiology of Disease |
|
| Company Name: |
Wuhan Topule
|
| Tel: |
+86-02787215551 +86-19945035818 |
| Website: |
http://www.topule.com/ |
|