532813 p21 Inhibitor, UC2288 - Calbiochem

532813
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₀H₁₈ClF₆N₃O₂

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      5.32813.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable, orally available, phenylcyclohexyl-urea based compound that selectively downregulates the expression of p21 (~10 µM), independent of p53 expression, at either transcription or post-transcriptional level. However, it does not affect the stability of p21. Also, it has no significant effect on the activities of Raf kinases, VEGFR2 kinase, or the phosphorylation state of ERK. Effectively blocks the growth of multiple cancer cell lines (GI50 ~ 10 µM against NCI60 cell lines). Its greater inhibitory effect on cytosolic p21 is indicative of its ability to induce apoptotic cell death in 786-O cells. Synergistically suppresses the growth of HCT116 and ACHN cells in athymic nude mice when combined with imetelstat, a telomerase inhibitor (15 mg/kg of UC2288, p.o., & 30 mg/kg of imetelstat, i.p., 3 times per week).

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number532813
          Brand Family Calbiochem®
          Synonyms1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-((1r,4r)-4-(5-(trifluoromethyl)pyridin-2-yloxy)cyclohexyl)urea, trans-1-(4-Chloro-3-trifluoromethyl-phenyl)-3-(4-hydroxy-cyclohexyl)-urea, p21/Cip1/CKI/Waf1 Inhibitor, t-CTTU; UC-2288
          References
          ReferencesGupta, R., et al. 2014. Proc. Natl. Acad. Sci. USA 111, E3062.
          Wettersten, H.I., et al. 2013. Cancer Biol. Ther. 14, 278.
          Product Information
          FormWhite solid
          Hill FormulaC₂₀H₁₈ClF₆N₃O₂
          Chemical formulaC₂₀H₁₈ClF₆N₃O₂
          Quality LevelMQ100
          Applications
          Biological Information
          Purity≥98% by HPLC
          Physicochemical Information
          Cell permeableY
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          p21 Inhibitor, UC2288 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          p21 Inhibitor, UC2288 - Calbiochem Certificates of Analysis

          TitleLot Number
          532813

          References

          Reference overview
          Gupta, R., et al. 2014. Proc. Natl. Acad. Sci. USA 111, E3062.
          Wettersten, H.I., et al. 2013. Cancer Biol. Ther. 14, 278.

          Technical Info

          Title
          Characterization of Estrogen Receptor α Phosphorylation Sites in Breast Cancer Tissue Using the SNAP i.d® 2.0 System
          White Paper: Further considerations of antibody validation and usage. (EMD)
          Data Sheet

          Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

          Revision15-March-2015 JSW
          Synonyms1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-((1r,4r)-4-(5-(trifluoromethyl)pyridin-2-yloxy)cyclohexyl)urea, trans-1-(4-Chloro-3-trifluoromethyl-phenyl)-3-(4-hydroxy-cyclohexyl)-urea, p21/Cip1/CKI/Waf1 Inhibitor, t-CTTU; UC-2288
          DescriptionA cell-permeable phenylcyclohexyl-urea compound that downregulates cellular p21/Cip1/CKI/Waf1 protein level (by > 95% in HCT116 cells after 24 h UC2288 treatment at 2.5 µM), presumably by means of a yet undetermined transcriptional or post-transcriptional regulation without affecting p21 cellular half-life or inhibiting the kinase activities of C-raf, B-rafV600E, or VEGFR2 (IC50 > 10 µM). Dual telomerase and p21, but not p16 or p27 (gene = CDKN1A, CDKN2A, CDKN1B, respectively), knockdown/inhibition is demonstrated to effectively kill cancer cells both in vitro (% viability inhibition/% Annexin V+ cells induction = 20%/2% or 77%/55%, respectively, following telomerase inhibition by Imetelstat with or without 2.5 µM UC2288 for 24 h in HCT116 colon cancer cultures) and in mice in vivo (% tumor expansion suppression by UC2288 alone/Imetelstat alone/combined treatment = 13%/42%/90%/HCT116 and 4%/23%/92%/ACHN; 30 mg Imetelstat/kg via i.p. and/or 15 mg UC2288/kg via p.o. 3X/wk for 3 wk) by inducing p53- and E2F1-dependent PUMA expression, while p21 overexpression, p53 inactivation by mutation, shRNA-mediated E2F1 or PUMA downregulation abolishes such synergized cell killing. Likewise, reactivating mutant p53 activitiy by CP-31398 (Cat. No. 506166) treatment is reported to resensitize DLD1 (p53 S241F) and A375.S2 (p53 R273H & P309S) to p21 shRNA- & Imetelstat-induced apoptotic cell death and tumor growth inhibition.
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₀H₁₈ClF₆N₃O₂
          Purity≥98% by HPLC
          SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesGupta, R., et al. 2014. Proc. Natl. Acad. Sci. USA 111, E3062.
          Wettersten, H.I., et al. 2013. Cancer Biol. Ther. 14, 278.