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500713 EphA Antagonist - CAS 674782-30-0 - Calbiochem

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

Synonyms: 4-(2,5-dimethyl-1H-pyrrol-1-yl)-2-hydroxybenzoic acid, EphA2 Antagonist, EphA4 Antagoinst, Ephrin Receptor Antagonist, Rtk2 Antagonist, Rtk1 Antagonist

Primary Target: EphA
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
674782-30-0C₁₃H₁₃NO₃

Products

Catalog NumberPackaging Qty/Pack
5.00713.0001 Glass bottle 10 mg
Description
OverviewA pyrrolyl benzoic acid that effectively competes against ephrin-B3 for EphA4 binding as well as against ephrin-A1/-A2/-A3/-A5 for EphA2 and EphA4 binding by targeting EphA2/A4 high affinity ephrin-binding pocket in a reversible manner, exhibiting much reduced or no potency against ephrin-A4 for EphA2/EphA4 binding, ephrin-A5 for EphA3/A5/A6/A7 binding, ephrin-B2 for B1/B2/B3/B4/B6 binding, or ephrin-B2 for EphA4 binding. Shown to inhibit ephrin-A1-induced EphA2 phosphorylation (by 92% at 200 µM) and ephrin-A5-induced EphA4 phosphorylation (by 79% at 400 µM) in cultures in vitro and prevent ephrin-A5-induced growth cone collapse of neurons in 6-d chicken embryo retina (by 100% at 400 µM) ex vivo, as well as rescue human mutant SOD-1 A4V transgene-induced axonopathy in zebrafish embryos (500 µM from 6 to 30 hpf) in vivo.
Catalogue Number500713
Brand Family Calbiochem®
Synonyms4-(2,5-dimethyl-1H-pyrrol-1-yl)-2-hydroxybenzoic acid, EphA2 Antagonist, EphA4 Antagoinst, Ephrin Receptor Antagonist, Rtk2 Antagonist, Rtk1 Antagonist
References
ReferencesVan Hoecke, A., et al. 2012. Nat. Med. 18, 1418.
Noberini, R., et al. 2008. J. Biol. Chem. 283, 29461.
Product Information
CAS number674782-30-0
FormOrange powder
Hill FormulaC₁₃H₁₃NO₃
Chemical formulaC₁₃H₁₃NO₃
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetEphA
Primary Target IC<sub>50</sub>3 micro
Purity≥95% by HPLC
Physicochemical Information
Cell permeableN
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 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 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
5.00713.0001 04055977264227

Documentation

EphA Antagonist - CAS 674782-30-0 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Van Hoecke, A., et al. 2012. Nat. Med. 18, 1418.
Noberini, R., et al. 2008. J. Biol. Chem. 283, 29461.
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.

Revision21-June-2013 JSW
Synonyms4-(2,5-dimethyl-1H-pyrrol-1-yl)-2-hydroxybenzoic acid, EphA2 Antagonist, EphA4 Antagoinst, Ephrin Receptor Antagonist, Rtk2 Antagonist, Rtk1 Antagonist
DescriptionA pyrrolyl benzoic acid that effectively competes against ephrin-B3 for EphA4 binding as well as against ephrin-A1/-A2/-A3/-A5 for EphA2 and EphA4 binding by targeting EphA2/A4 high affinity ephrin-binding pocket in a reversible manner (Ki = 6-10 and 11-14 µM against ephrin-A5 binding to EphA4 and EphA2, respectively), exhibiting much reduced or no potency against ephrin-A4 for EphA2/EphA4 binding, ephrin-A5 for EphA3/A5/A6/A7 binding, ephrin-B2 for B1/B2/B3/B4/B6 binding, or ephrin-B2 for EphA4 binding. Shown to inhibit 0.1 µg/mL ephrin-A1-Fc fusion-induced EphA2 phosphorylation in COS7 (by 92% at 200 µM) and 0.5 µg/mL ephrin-A5-Fc fusion-induced EphA4 phosphorylation in HT22 neuronal cultures (by 42% and 79% respectively, at 300 and 400 µM) without any cytotoxicity (up to 400 µM and 3 days in HT22 cultures). Also effective toward chicken and zebrafish EphA4 orthologs as evidenced by its efficacy in preventing 1 µg/mL ephrin-A5-Fc-induced growth cone collapse of neurons in 6-d chicken embryo retina (by 100% at 400 µM) ex vivo and in fully rescuing human mutant SOD-1 A4V transgene-induced axonopathy in zebrafish embryos (500 µM; treatment period from 6 to 30 hpf) in vivo.
FormOrange powder
Intert gas (Yes/No) Packaged under inert gas
CAS number674782-30-0
Chemical formulaC₁₃H₁₃NO₃
Structure formulaStructure formula
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 3 months at -20°C.
Toxicity Standard Handling
ReferencesVan Hoecke, A., et al. 2012. Nat. Med. 18, 1418.
Noberini, R., et al. 2008. J. Biol. Chem. 283, 29461.