676503 | VEGFR/Tie-2/PDGFR Tyrosine Kinase Inhibitor - Calbiochem

676503
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₂₁H₁₅F₄N₅O₂

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      676503-5MG
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      Limited AvailabilityLimited Availability
      In Stock 
      Discontinued
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          Glass bottle 5 mg
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          Description
          OverviewAn orally bioavailable pyrrolopyrimidinylurea compound that simultaneously binds to both the adenine and the adjacent hydrophobic pocket of the inactive form of VEGFR2 with high-affinity (type-II inhibitor) and acts as a pseudo-irreversible inhibitor with prolonged action. Shown to potently inhibit the activities of VEGFR2, VEGFR1, Tie-2, PDGFRα, PDGFRβ and c-kit (IC50 = 6.2, 15, 20, 35, 96 and 170 nM, respectively) with moderate to excellent selectivity over B-raf and Aurora-A (IC50 = 0.9 and 1.05 µM) and FGFR1, HER2, EGFR, IR, PKCθ (> 10 µM) among 18-kinases. Arrests VEGF-induced HUVECs proliferation (IC50 = 4.4 µM) and suppresses DU145 carcinoma growth in a xenograft nude mouse model (6 mg/kg, b.i.d.).
          Catalogue Number676503
          Brand Family Calbiochem®
          Synonyms1-(2-Fluoro-4-((5-methyl-5H-pyrrolo[3,2-d]pyrimidin-4-yl)oxy)phenyl)-3-(3-(trifluoromethyl)phenyl)urea, VEGFR Tyrosine Kinase Inhibitor XXXIV, VEGFR2 Kinase Inhibitor XXXII, VEGFR1 Kinase Inhibitor VII, PDGFR Tyrosine Kinase Inhibitor XXI
          References
          ReferencesOguro, Y., et al. 2010. Bioorg. Med. Chem. 18, 7150.
          Product Information
          FormLight beige solid
          Hill FormulaC₂₁H₁₅F₄N₅O₂
          Chemical formulaC₂₁H₁₅F₄N₅O₂
          Hygroscopic Hygroscopic
          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 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
          Hygroscopic Hygroscopic
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 monthst at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          676503

          References

          Reference overview
          Oguro, Y., et al. 2010. Bioorg. Med. Chem. 18, 7150.
          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-September-2012 JSW
          Synonyms1-(2-Fluoro-4-((5-methyl-5H-pyrrolo[3,2-d]pyrimidin-4-yl)oxy)phenyl)-3-(3-(trifluoromethyl)phenyl)urea, VEGFR Tyrosine Kinase Inhibitor XXXIV, VEGFR2 Kinase Inhibitor XXXII, VEGFR1 Kinase Inhibitor VII, PDGFR Tyrosine Kinase Inhibitor XXI
          DescriptionAn orally bioavailable pyrrolopyrimidinylurea compound that simultaneously binds to both the adenine and the adjacent hydrophobic pocket of the inactive form of VEGFR2 with high-affinity (type-II inhibitor) and acts as a pseudo-irreversible inhibitor with prolonged action. Shown to potently inhibit the activities of VEGFR2, VEGFR1, Tie-2, PDGFRα, PDGFRβ and c-kit (IC50 = 6.2, 15, 20, 35, 96 and 170 nM, respectively) with moderate to excellent selectivity over B-raf and Aurora-A (IC50 = 0.9 and 1.05 µM) and FGFR1, HER2, EGFR, IR, PKCθ (> 10 µM) among 18-kinases. Arrests VEGF-induced HUVECs proliferation (IC50 = 4.4 µM) and suppresses DU145 carcinoma growth in a xenograft nude mouse model (6 mg/kg, b.i.d.).
          FormLight beige solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₁H₁₅F₄N₅O₂
          Purity≥95% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          Hygroscopic
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 monthst at -20°C.
          Toxicity Standard Handling
          ReferencesOguro, Y., et al. 2010. Bioorg. Med. Chem. 18, 7150.