419820 | ITK Inhibitor, BMS-509744 - CAS 439575-02-7 - Calbiochem

419820
Price could not be retrieved
Minimum Quantity needs to be mulitiple of
Upon Order Completion More Information
You Saved ()
 
Request Pricing
Limited AvailabilityLimited Availability
Stocked 
Discontinued
Limited Quantities Available
Available
    Remaining : Will advise
      Remaining : Will advise
      Will advise
      Contact Customer Service
      View Pricing & Availability
      Click To Print This Page

      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₃₂H₄₁N₅O₄S₂ 439575-02-7

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      419820-5MG
      Retrieving availability...
      Limited AvailabilityLimited Availability
      Stocked 
      Discontinued
      Limited Quantities Available
      Available
        Remaining : Will advise
          Remaining : Will advise
          Will advise
          Contact Customer Service

          Glass bottle 5 mg
          Retrieving price...
          Price could not be retrieved
          Minimum Quantity needs to be mulitiple of
          Upon Order Completion More Information
          You Saved ()
           
          Request Pricing
          Description
          OverviewA cell-permeable aminothioaryl-thiazolo compound that potently inhibits ITK kinase activity (IC50 = 19 nM; [ATP] = 1 µM) in an ATP-competitive manner by stabilizing ITK activation loop in a substrate-blocking, inactive conformation, inhibiting Fyn, IR, Lck, Btk only at much higher concentrations (IC50 ≥1.1 µM) and exhibiting little or no activity against 14 other kinases (IC50 ≥11 µM). Inhibits ITK-dependent cellular signaling (IC50 <300 nM against αCD3-stimulated PLCγ1 Tyr phosphorylation and Ca2+ mobilization in Jurkat cells) in vitro and alleviate OVA (Cat. No. 32467) challenge-induced airway leukocytes infiltration (ED50 = 25 mg/kg s.c.) in OVA-sensitized mice in vivo.
          Catalogue Number419820
          Brand Family Calbiochem®
          SynonymsBMS509744; EMT Inhibitor, IL-2-Inducible T Cell Kinase Inhibitor, N-(5-(5-(4-Acetylpiperazine-1-carbonyl)-4-methoxy-2-methylphenylthio)thiazol-2-yl)-4-((3,3-dimethylbutan-2-ylamino)methyl)benzamide, N-(5-((3-((4-Acetylpiperazin-1-yl)carbonyl)-4-methyl-6-methoxyphenyl)thio)thiazol-2-yl)-4-(N-1,2-dimethylpropylaminomethyl)benzamide
          References
          ReferencesKutach, A.K., et al. 2010. Chem. Biol. Drug Des. 76, 154.
          Das, J., et al. 2006. Bioorg. Med. Chem. Lett. 16, 3706.
          Lin, T.A., et al. 2004. Biochemistry 43, 11056.
          Product Information
          CAS number439575-02-7
          FormPale yellow powder
          Hill FormulaC₃₂H₄₁N₅O₄S₂
          Chemical formulaC₃₂H₄₁N₅O₄S₂
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetITK
          Primary Target IC<sub>50</sub>19 nM for ITK
          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 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          Certificates of Analysis

          TitleLot Number
          419820

          References

          Reference overview
          Kutach, A.K., et al. 2010. Chem. Biol. Drug Des. 76, 154.
          Das, J., et al. 2006. Bioorg. Med. Chem. Lett. 16, 3706.
          Lin, T.A., et al. 2004. Biochemistry 43, 11056.
          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.

          Revision22-February-2013 JSW
          SynonymsBMS509744; EMT Inhibitor, IL-2-Inducible T Cell Kinase Inhibitor, N-(5-(5-(4-Acetylpiperazine-1-carbonyl)-4-methoxy-2-methylphenylthio)thiazol-2-yl)-4-((3,3-dimethylbutan-2-ylamino)methyl)benzamide, N-(5-((3-((4-Acetylpiperazin-1-yl)carbonyl)-4-methyl-6-methoxyphenyl)thio)thiazol-2-yl)-4-(N-1,2-dimethylpropylaminomethyl)benzamide
          DescriptionA cell-permeable aminothioaryl-thiazolo compound that potently inhibits ITK kinase activity (IC50 = 19 nM; [ATP] = 1 µM) in an ATP-competitive manner by stabilizing ITK activation loop in a substrate-blocking, inactive conformation, inhibiting Fyn, IR, Lck, Btk only at much higher concentrations (IC50 = 1.1, 1.1, 2.4, and 4.1 µM, respectively) and exhibiting little or no activity against 14 other kinases (IC50 ≥11 µM). Inhibits ITK-dependent, but not ITK-independent, PLCγ1 tyrosine phosphorylation (IC50 <300 nM in αCD3-stimulated Jurkat T-cells) as well as downstream signaling events, including Ca2+ mobilization (IC50 = 52 nM in αCD3-stimulated Jurkat T-cells), IL-2 secretion (IC50 = 72, 250, 380, and 390 nM, respectively, in αCD3-stimulated EL4, Jurkat, murine splenocytes, and human PBMCs), and proliferation (IC50 = 430 nM against APC-induced primary human T-cell expansion). BMS-509744 is also efficacious in alleviating OVA (Cat. No. 32467) challenge-induced airway leukocytes infiltration (50% and 75% reduction, respectively, of total and eosinophil cell count; 25 mg/kg s.c.) in OVA- sensitized mice in vivo.
          FormPale yellow powder
          Intert gas (Yes/No) Packaged under inert gas
          CAS number439575-02-7
          Chemical formulaC₃₂H₄₁N₅O₄S₂
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (100 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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesKutach, A.K., et al. 2010. Chem. Biol. Drug Des. 76, 154.
          Das, J., et al. 2006. Bioorg. Med. Chem. Lett. 16, 3706.
          Lin, T.A., et al. 2004. Biochemistry 43, 11056.