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

A cell-permeable compound that downregulates cellular BMI-1 levels by inhibiting BMI-1 transcription.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: FLVI2/BMI1 Expression Inhibitor, MGC12685 Expression Inhibitor, PCGF4 Expression Inhibitor, PTC209; RNF51 Expression Inhibitor

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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
315704-66-6C₁₇H₁₃Br₂N₅OS

Products

Catalogue NumberPackaging Qty/Pack
5.30154.0001 Glass bottle 10 mg
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
Global Trade Item Number
Catalogue Number GTIN
5.30154.0001 04055977241259

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 Protect from light
+2°C to +8°C
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.