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100082 14-3-3 Antagonist II, BV02 - Calbiochem

100082
  
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Áttekintés

Replacement Information

Kulcsspecifikációk táblázata

Empirical Formula
C₂₀H₁₇N₃O₆
Description
Overview

This product has been discontinued.



A cell-permeable, non-peptidyl pyrazolylcarbamoyl compound that targets the amphipathic client protein-binding groove of 14-3-3 and effectively competes against cellular pro-apoptotic c-Abl and cell cycle inhibitor protein p27Kip1 (CDK inhibitor 1B) for 14-3-3ς interaction, leading to c-Abl mitochondrial membrane relocation, c-Abl and p27Kip1 nuclear translocation, sub-G1 arrest, enhanced c-Abl cleavage, caspase-9 and -8 activation (24 h 5 µM treatment), and eventual apoptotic cell death in pro-B murine Ba/F3 lines expressing wt, E255K, or T315I Bcr-Abl (LD50 = 0.41, 1.30, 1.47 µM, respectively;). Also demonstrated to exhibit antiproliferative activity against the survival of three primary IM- (Imatinib mesylate; STI571) resistant CD34+ cultures (LD50 = 0.5, 0.7, and 2.5 µM) from CML (chronic myeloid leukemia) patients with T315I Bcr-Abl mutation.

Catalogue Number100082
Brand Family Calbiochem®
Synonyms2-(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-ylcarbamoyl)terephthalic acid
References
ReferencesMancini, M., et al. 2011. J. Pharmacol. Exp. Ther. 336, 596.
Product Information
FormOff-white powder
Hill FormulaC₂₀H₁₇N₃O₆
Chemical formulaC₂₀H₁₇N₃O₆
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥98% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Regulatory Review
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

14-3-3 Antagonist II, BV02 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

14-3-3 Antagonist II, BV02 - Calbiochem Certificates of Analysis

TitleLot Number
100082

References

Hivatkozások áttekintése
Mancini, M., et al. 2011. J. Pharmacol. Exp. Ther. 336, 596.
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.

Revision02-April-2012 JSW
Synonyms2-(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-ylcarbamoyl)terephthalic acid
DescriptionA cell-permeable, non-peptidyl pyrazolylcarbamoyl compound that targets the amphipathic client protein-binding groove of 14-3-3 and effectively competes against cellular pro-apoptotic c-Abl and cell cycle inhibitor protein p27Kip1 (CDK inhibitor 1B) for 14-3-3ς interaction, leading to c-Abl mitochondrial membrane relocation, c-Abl and p27Kip1 nuclear translocation, sub-G1 arrest, enhanced c-Abl cleavage, caspase-9 and -8 activation (24 h 5 µM treatment), and eventual apoptotic cell death in pro-B murine Ba/F3 lines expressing wt, E255K, or T315I Bcr-Abl (LD50 = 0.41, 1.30, 1.47 µM, respectively;). Also demonstrated to exhibit antiproliferative activity against the survival of three primary IM- (Imatinib mesylate; STI571) resistant CD34+ cultures (LD50 = 0.5, 0.7, and 2.5 µM) from CML (chronic myeloid leukemia) patients with T315I Bcr-Abl mutation.
FormOff-white powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₀H₁₇N₃O₆
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (5 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 Regulatory Review
ReferencesMancini, M., et al. 2011. J. Pharmacol. Exp. Ther. 336, 596.