UC2288
UC2288 Basic information
- Product Name:
- UC2288
- 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
- Urea, N-[4-chloro-3-(trifluoromethyl)phenyl]-N'-[trans-4-[[5-(trifluoromethyl)-2-pyridinyl]oxy]cyclohexyl]-
- UC 2288, trans
- 1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(trans-4-((5-(trifluoromethyl)pyridin-2-yl)oxy)cyclohexyl)urea , UC2288
- UC2288, p21 inhibitor
- UC2288, 10 mM in DMSO
- CAS:
- 1394011-91-6
- MF:
- C20H18ClF6N3O2
- MW:
- 481.82
- Mol File:
- 1394011-91-6.mol
UC2288 Chemical Properties
- 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
UC2288 Usage And Synthesis
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
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