428201 LDN-211904 - Calbiochem

428201
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₁H₂₁ClN₄O₅

Pricing & Availability

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428201-5MG
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      Glass bottle 5 mg
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      Description
      OverviewA pyrazolo[1,5-a]pyridine derivative that acts as an potent and reversible EphB3 receptor tyrosine kinase inhibitor with an IC50 of 79 nM with good mouse liver microsomal stability and aqueous solubility. Shown to suppress EphB3-induced autophosphorylation of EphB3 receptor at 10 µM in cells. When profiled against a panel of 288 kinases at 5 µM, found to also inhibit most of the Eph (Erythropoietin-producing hepatocellular carcinoma) receptor kinases including EphA1, EphA2, EphA3, EphA4, EphA5, EphA8, EphB1, EphB2, EphB3, EphB4 and other tyrosine kinases, but not EphA6 and EphA7, and is non-inhibitory towards non-RTK kinases screened except for p38α, p38β, and Qik.
      Catalogue Number428201
      Brand Family Calbiochem®
      SynonymsEphB3 inhibitor, LDN-211904, N-(2-chlorophenyl)-6-(piperidin-4-yl)imidazo[1,2-a]pyridine-3-carboxamide oxalate
      References
      ReferencesQiao, L., et al. 2011, Bioorg. Med. Chem. Lett. 19, 6122
      Product Information
      FormOff-white solid
      Hill FormulaC₂₁H₂₁ClN₄O₅
      Chemical formulaC₂₁H₂₁ClN₄O₅
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetErythropoietin-producing hepatocellular carcinoma (Eph)
      Primary Target IC<sub>50</sub>79 nM
      Purity≥99% 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 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
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      LDN-211904 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      LDN-211904 - Calbiochem Certificates of Analysis

      TitleLot Number
      428201

      References

      Reference overview
      Qiao, L., et al. 2011, Bioorg. Med. Chem. Lett. 19, 6122
      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.

      Revision09-July-2012 JSW
      SynonymsEphB3 inhibitor, LDN-211904, N-(2-chlorophenyl)-6-(piperidin-4-yl)imidazo[1,2-a]pyridine-3-carboxamide oxalate
      DescriptionA pyrazolo[1,5-a]pyridine derivative that acts as an potent and reversible EphB3 receptor tyrosine kinase inhibitor with an IC50 of 79 nM with good mouse liver microsomal stability and aqueous solubility. Shown to suppress EphB3-induced autophosphorylation of EphB3 receptor at 10 µM in cells. When profiled against a panel of 288 kinases at 5 µM, found to also inhibit most of the Eph (Erythropoietin-producing hepatocellular carcinoma) receptor kinases including EphA1, EphA2, EphA3, EphA4, EphA5, EphA8, EphB1, EphB2, EphB3, EphB4 and other tyrosine kinases, but not EphA6 and EphA7, and is non-inhibitory towards non-RTK kinases screened except for p38α, p38β, and Qik.
      FormOff-white solid
      Chemical formulaC₂₁H₂₁ClN₄O₅
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (50 mg/ml; clear, nearly colorless solution)
      Storage +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesQiao, L., et al. 2011, Bioorg. Med. Chem. Lett. 19, 6122