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330000 ESFTs Inhibitor, YK-4-279

ESFTs Inhibitor, YK-4-279 MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 4,7-Dichloro-3-hydroxy-3-(2-(4-methoxyphenyl)-2-oxoethyl)-1,3-dihydro-2H-indol-2-one, EWS-FLI1 Inhibitor

330000
  
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₇H₁₃Cl₂NO₄
Description
Overview

This product has been discontinued.



A cell-permeable dihydroindolone compound that disrupts the Ewing's sarcoma oncogenic transcription factor, EWS-FLI1, complex assembly by competing against RHA (RNA helicase A) binding to EWS-FLI1 (KD = 9.48 µM) and inhibits EWS-FLI1-dependent transcription activity (by 76% and 88% in 18 h with 3 and 10 µM YK-4-279, respectively) in COS7-based reporter assays without affecting NF-κB-mediated transcription even at concentrations as high as 10 µM. Shown to exhibit apoptosis-inducing and antiproliferative activity toward ESFT (Ewing's sarcoma family tumor) cells both in cultures in vitro (IC50 between 0.5 and 8.0 µM) and in mice in vivo (Average tumor growth retardation >50% on day 14; Three 1.5 mg i.p. doses/mouse/day), while displaying little or much reduced activity toward non-EWS-FLI1 cancer cells or nontransformed cells (IC50 ≥25 µM).
Catalogue Number330000
Brand Family Calbiochem®
Synonyms4,7-Dichloro-3-hydroxy-3-(2-(4-methoxyphenyl)-2-oxoethyl)-1,3-dihydro-2H-indol-2-one, EWS-FLI1 Inhibitor
References
ReferencesErkizan, H.V., et al. 2009. Nature Med. 15, 750.
Product Information
FormTan solid
Hill FormulaC₁₇H₁₃Cl₂NO₄
Chemical formulaC₁₇H₁₃Cl₂NO₄
Structure formula ImageStructure formula Image
Applications
Biological Information
Purity≥95% by HPLC
Physicochemical Information
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 -20°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 3 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
330000 0

Documentation

ESFTs Inhibitor, YK-4-279 Certificates of Analysis

TitleLot Number
330000

References

Reference overview
Erkizan, H.V., et al. 2009. Nature Med. 15, 750.
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.

Revision28-February-2011 RFH
Synonyms4,7-Dichloro-3-hydroxy-3-(2-(4-methoxyphenyl)-2-oxoethyl)-1,3-dihydro-2H-indol-2-one, EWS-FLI1 Inhibitor
DescriptionA cell-permeable dihydroindolone compound that disrupts the Ewing's sarcoma oncogenic transcription factor, EWS-FLI1, complex assembly by competing against RHA (RNA helicase A) binding to EWS-FLI1 (KD = 9.48 µM) and inhibits EWS-FLI1-dependent transcription activity (by 76% and 88% in 18 h with 3 and 10 µM YK-4-279, respectively) in COS7-based reporter assays without affecting NF-κB-mediated transcription even at concentrations as high as 10 µM. Shown to exhibit apoptosis-inducing and antiproliferative activity toward ESFT (Ewing's sarcoma family tumor) cells both in cultures in vitro (IC50 between 0.5 and 8.0 µM) and in mice in vivo (Average tumor growth retardation >50% on day 14; Three 1.5 mg i.p. doses/mouse/day), while displaying little or much reduced activity toward non-EWS-FLI1 cancer cells or nontransformed cells (IC50 ≥25 µM).
FormTan solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₇H₁₃Cl₂NO₄
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesErkizan, H.V., et al. 2009. Nature Med. 15, 750.