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

530154
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Empirical FormulaCAS #
C₁₇H₁₃Br₂N₅OS 315704-66-6

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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
      Quality LevelMQ100
      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.