530154 BMI-1 Expression Inhibitor, PTC-209 - CAS 315704-66-6 - Calbiochem

530154
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₇H₁₃Br₂N₅OS 315704-66-6

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      5.30154.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable imidazopyrimidinyl-thiazolamine compound that effectively downregulates cellular BMI-1 protein level both in cultures in vitro (IC50 = 0.5 µM/48 h/HT1080 and <0.37 µM/HCT116/overnight) and in mice in vivo (60 mg/kg/d via s.c.) by inhibiting BMI-1 transcription via a yet unidentified mechanism, thereby reducing BMI-1-dependent RING1A E3 ligase activity and RING1A-mediated H2A ubiquitination (uH2A)/epigenetic regulations. Shown to exhibit antiproliferation activity against human colon cancer cells both in cultures (IC50 <300 nM) in vitro and in mice (30 to 60 mg/kg/d s.c.) in vivo via G0 cell cycle arrest and apoptosis induction with a greater drug impact on self-renewing cancer-initiating cells (CICs; cancer stem cells).
          Catalogue Number530154
          Brand Family Calbiochem®
          SynonymsFLVI2/BMI1 Expression Inhibitor, MGC12685 Expression Inhibitor, PCGF4 Expression Inhibitor, PTC209; RNF51 Expression Inhibitor
          References
          ReferencesKreso, A., et al. 2014. Nat. Med. 20, 29.
          Product Information
          CAS number315704-66-6
          FormLight yellow powder
          Hill FormulaC₁₇H₁₃Br₂N₅OS
          Chemical formulaC₁₇H₁₃Br₂N₅OS
          ReversibleN
          Applications
          Biological Information
          Purity≥95% 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

          BMI-1 Expression Inhibitor, PTC-209 - CAS 315704-66-6 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Kreso, A., et al. 2014. Nat. Med. 20, 29.
          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.

          Revision08-May-2014 JSW
          SynonymsFLVI2/BMI1 Expression Inhibitor, MGC12685 Expression Inhibitor, PCGF4 Expression Inhibitor, PTC209; RNF51 Expression Inhibitor
          DescriptionA cell-permeable imidazopyrimidinyl-thiazolamine compound that effectively downregulates cellular BMI-1 protein level both in cultures in vitro (IC50 = 0.5 µM/48 h/HT1080 and <0.37 µM/HCT116/overnight) and in mice in vivo (4.5 ng vs.13.7 ng per mg HT1080 tumor tissue, respectively, with or without 10-d 60 mg/kg/d treatment via s.c.) by inhibiting BMI-1 transcription (IC50 = 0.5 µM against overnight reporter transcription in HEK293) via a yet unidentified mechanism, thereby reducing BMI-1-dependent RING1A E3 ligase activity and RING1A-mediated H2A ubiquitination (uH2A)/epigenetic regulations. Shown to exhibit antiproliferation activity against human colon cancer cells both in cultures (IC50 <300 nM against LS174T and primary colon cancer cultures) in vitro and in mice (30 to 60 mg/kg/d s.c.) in vivo by inducing cell cycle arrest at G0 and apoptosis. Reduced frequency of sphere-forming cells is observed among surviving cells (by 1.7- to 2.2-fold) upon PTC-209 removal post a 4-day 0.1 µM drug treatment period in primary colon cancer cultures, indicating a greater impact of drug treatment on self-renewing cancer-initiating cells (CICs; cancer stem cells). Likewise, surviving colon cancer cells from tumor-bearing mice at the end of drug treatment are shown to contain reduced population of tumor-initiating cells when xenografted into secondary recipient mice.
          FormLight yellow powder
          Intert gas (Yes/No) Packaged under inert gas
          CAS number315704-66-6
          Chemical formulaC₁₇H₁₃Br₂N₅OS
          Purity≥95% by HPLC
          SolubilityDMSO (100 mg/ml)
          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
          ReferencesKreso, A., et al. 2014. Nat. Med. 20, 29.