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530615 GFRα/RET Signaling Activator, XIB-4035 - CAS 10023-54-8 - Calbiochem

A cell-permeable compound that competitively binds to GFRα1 and act as an agonist (IC₅₀ = 10.4 µM for 125I-GDNF binding in Neuro-2A cells) to induce autophosphorylation of RET protein.

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

Synonyms: (E)-N⁴-(7-Chloro-2-(2-chlorostyryl)quinolin-4-yl)-N¹,N¹-diethylpentane-1,4-diamine, N-(7-Chloro-2-(2-(2-chlorophenyl)vinyl)-4-quinolinyl)-N-(4-(diethylamino)-1-methylbutyl)amine, XIB 4035

Primary Target: GFRα1
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      Overview

      Replacement Information

      Key Specifications Table

      CAS #Empirical Formula
      10023-54-8C₂₆H₃₁Cl₂N₃
      Description
      OverviewA cell-permeable chlorostyrylquinolinylbutylamino compound that was shown to competitively bind to glial cell line-derived neurotrophic factor (GDNF) family receptor-α1 (GFRα1) and act as an agonist (IC50 = 10.4 µM for 125I-GDNF binding in Neuro-2A cells) and induce autophosphorylation of RET protein. Elicits neurite outgrowth of Neuro-2A cells in a dose-dependent manner. However, some of the recent studies have questioned its agonist nature and have suggested that it acts as a positive modulator of ligand-Induced GFRα/RET signaling and prolongs the GDNF-induced RET phosphorylation. Shown to be effective in treating small fiber neuropathy caused by non-myelinating Schwann cell dysfunction in diabetic murine models leading to improved thermononiception. Does not appear to be toxic up to ~100 µM.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number530615
      Brand Family Calbiochem®
      Synonyms(E)-N⁴-(7-Chloro-2-(2-chlorostyryl)quinolin-4-yl)-N¹,N¹-diethylpentane-1,4-diamine, N-(7-Chloro-2-(2-(2-chlorophenyl)vinyl)-4-quinolinyl)-N-(4-(diethylamino)-1-methylbutyl)amine, XIB 4035
      References
      ReferencesHedstrom, K.L., et al. 2014. Proc. Natl. Acad. Sci. USA 111, 2325.
      Tokugawa, K., et al. 2003. Neurochem. Int. 42, 81.
      Product Information
      CAS number10023-54-8
      FormYellow powder
      Hill FormulaC₂₆H₃₁Cl₂N₃
      Chemical formulaC₂₆H₃₁Cl₂N₃
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetGFRα1
      Primary Target IC<sub>50</sub>10.4 µM for ¹²⁵I-GDNF binding in Neuro-2A cells
      Purity≥97% 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 -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 Identification Number
      Catalog Number GTIN
      530615

      Documentation

      GFRα/RET Signaling Activator, XIB-4035 - CAS 10023-54-8 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Hedstrom, K.L., et al. 2014. Proc. Natl. Acad. Sci. USA 111, 2325.
      Tokugawa, K., et al. 2003. Neurochem. Int. 42, 81.
      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.

      Revision20-June-2014 JSW
      Synonyms(E)-N⁴-(7-Chloro-2-(2-chlorostyryl)quinolin-4-yl)-N¹,N¹-diethylpentane-1,4-diamine, N-(7-Chloro-2-(2-(2-chlorophenyl)vinyl)-4-quinolinyl)-N-(4-(diethylamino)-1-methylbutyl)amine, XIB 4035
      DescriptionA cell-permeable chlorostyrylquinolinylbutylamino compound that was shown to competitively bind to glial cell line-derived neurotrophic factor (GDNF) family receptor-α1 (GFRα1) and act as an agonist (IC50 = 10.4 µM for 125I-GDNF binding in Neuro-2A cells) and induce autophosphorylation of RET protein. Elicits neurite outgrowth of Neuro-2A cells in a dose-dependent manner. However, some of the recent studies have questioned its agonist nature and have suggested that it acts as a positive modulator of ligand-Induced GFRα/RET signaling and prolongs the GDNF-induced RET phosphorylation. Shown to be effective in treating small fiber neuropathy caused by non-myelinating Schwann cell dysfunction in diabetic murine models leading to improved thermononiception. Does not appear to be toxic up to ~100 µM.
      FormYellow powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number10023-54-8
      Chemical formulaC₂₆H₃₁Cl₂N₃
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
      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
      ReferencesHedstrom, K.L., et al. 2014. Proc. Natl. Acad. Sci. USA 111, 2325.
      Tokugawa, K., et al. 2003. Neurochem. Int. 42, 81.