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Purity: =98%
UC2288 is a novel, cell-permeable, orally bioavailable, potent and selective active p21 attenuator. UC2288 suppresses the growth of several other cancer cell lines as well as kidney cancer cell lines (GI50 = about 10 µM). This new p21 inhibitor will be crucial for understanding how p21 functions, and with more research, it might even find its way into the clinic.
| Targets |
p21
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|---|---|
| ln Vitro |
While it has no effect on other proteins, UC2288 (0-10 μM; 24 hours) lowers the levels of the protein p21 [1]. In a 24-hour period, UC2288 (0-10 μM) decreases p21 mRNA that is either anticipated or post-expressed, without affecting p53[1].
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| ln Vivo |
Imetelstat and UC2888 (peritoneal gavage; 15 mg/kg; three times per week; four weeks) can be given together to greatly slow the growth of tumors in mice without changing their body weight [2]. MPTP-treated mice exhibit less behavioral impairment and less MAPK activation in their brains when treated with UC2288 (ip; 10 mg/kg; 4 times on 7 days). In the brains of MPTP-treated mice, MPTP treatment raised levels of TNF-α, IL-6, and IL-1β; however, UC2288 significantly decreased MPTP-induced levels of TNF-α, IL-6, but not IL-1β. [3].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: HK2 (normal kidney), 786-O (RCC), Caki-1 (RCC), ACHN (RCC) and HEY (ovarian cancer) cell Tested Concentrations: 0 μM; ]. 1μM; 3μM; 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: diminished p21 protein expression. RT-PCR[1] Cell Types: p53 mutated RCC cell line 786-O Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Reduction of p21 mRNA, independent of p53 expression. |
| Animal Protocol |
Animal/Disease Models: Eightweeks old athymic nude mice (NCr nu/nu) were injected subcutaneously (sc) (sc) with HCT116 and ACHN cancer cells (2.5x106) [2]
Doses: 15 mg/kg Route of Administration: po (oral gavage); 3 times a week; 4 weeks ; Results of combined treatment with imetelstat: Combined treatment with imetelstat can synergistically inhibit tumor growth in mice. Animal/Disease Models: MPTP-induced C57BL6 Parkinson's disease mouse model [3] Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; 4 times within 7 days Experimental Results: Improved MPTP-induced PD progression by inhibiting neuroinflammation. |
| 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.
[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. [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 |
| Molecular Formula |
C₂₀H₁₈CLF₆N₃O₂
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|---|---|
| Molecular Weight |
481.82
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| Exact Mass |
481.10
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| Elemental Analysis |
C, 49.86; H, 3.77; Cl, 7.36; F, 23.66; N, 8.72; O, 6.64
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| CAS # |
1394011-91-6
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| Related CAS # |
1394011-91-6
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| Appearance |
Solid powder
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| SMILES |
C1CC(CCC1NC(=O)NC2=CC(=C(C=C2)Cl)C(F)(F)F)OC3=NC=C(C=C3)C(F)(F)F
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| InChi Key |
ISPSOOYSNVVMMB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H18ClF6N3O2/c21-16-7-4-13(9-15(16)20(25,26)27)30-18(31)29-12-2-5-14(6-3-12)32-17-8-1-11(10-28-17)19(22,23)24/h1,4,7-10,12,14H,2-3,5-6H2,(H2,29,30,31)
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| Chemical Name |
1-[4-chloro-3-(trifluoromethyl)phenyl]-3-[4-[5-(trifluoromethyl)pyridin-2-yl]oxycyclohexyl]urea
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| Synonyms |
UC-2288; UC-2288; UC2288
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 50~96 mg/mL (199.2~103.8 mM)
Ethanol: 12.5~21 mg/mL (25.9~43.6 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0755 mL | 10.3773 mL | 20.7546 mL | |
| 5 mM | 0.4151 mL | 2.0755 mL | 4.1509 mL | |
| 10 mM | 0.2075 mL | 1.0377 mL | 2.0755 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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