343021 | Flt-3 Inhibitor II - CAS 896138-40-2 - Calbiochem

343021
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₇H₁₂N₂O₃ 896138-40-2

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      343021-1MG
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          Plastic ampoule 1 mg
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          Description
          OverviewA cell-permeable symmetrical indolylmethanone kinase inhibitor that is more selective toward Flt3 over PDGFR either in cell-based receptor autophosphorylation (IC50 = 40 nM vs. 300 nM) or in cell-free kinase reactions (IC50 = 33 nM vs. 171 nM) and potently induces apoptosis in Flt3-expressing primary AML patient blasts. Affects Abl- or Kit-dependent cell growth only at much higher concentrations (IC50 = 4.2 and ≥0.5 µM, respectively), while exhibiting little effect against IL-3-mediated cellular signaling. The molecular mechanism of inhibition is presumably due to interaction at the enzyme's ATP-binding site.
          Catalogue Number343021
          Brand Family Calbiochem®
          SynonymsBis-(5-hydroxy-1H-indol-2-yl)methanone, PDGFR Tyrosine Kinase Inhibitor XI
          References
          ReferencesMahboobi, S., et al. 2006. J. Med. Chem. 49, 3101.
          Product Information
          CAS number896138-40-2
          ATP CompetitiveN
          FormYellowish brown solid
          Hill FormulaC₁₇H₁₂N₂O₃
          Chemical formulaC₁₇H₁₂N₂O₃
          ReversibleN
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetFlt-3
          Primary Target IC<sub>50</sub>40 nM against Flt3 in cell-based receptor autophosphorylation; 33 nM against Flt3 in cell-free kinase reactions
          Purity≥95% 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 Irritant
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          343021

          References

          Reference overview
          Mahboobi, S., et al. 2006. J. Med. Chem. 49, 3101.
          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.

          Revision14-September-2007 JSW
          SynonymsBis-(5-hydroxy-1H-indol-2-yl)methanone, PDGFR Tyrosine Kinase Inhibitor XI
          DescriptionA cell-permeable symmetrical indolylmethanone kinase inhibitor that is more selective toward Flt3 over PDGFR either in cell-based receptor autophosphorylation (IC50 = 40 nM vs. 300 nM) or in cell-free kinase reactions (IC50 = 33 nM vs. 171 nM) and potently induces apoptosis in Flt3-expressing primary AML patient blasts. Affects Abl- or Kit-dependent cell growth only at much higher concentrations (IC50 = 4.2 and ≥0.5 µM, respectively), while exhibiting little effect against IL-3-mediated cellular signaling. The molecular mechanism of inhibition is presumably due to interaction at the enzyme's ATP-binding site.
          FormYellowish brown solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number896138-40-2
          Chemical formulaC₁₇H₁₂N₂O₃
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (100 mg/ml) or Ethanol (5 mg/ml)
          Storage -20°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 Irritant
          ReferencesMahboobi, S., et al. 2006. J. Med. Chem. 49, 3101.