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565852 PTP Inhibitor XXXI, II-B08 - Calbiochem

PTP Inhibitor XXXI, II-B08, is a cell-permeable compound that targets SHP2 catalytic domain and inhibit SHP2-catalyzed pNPP hydrolysis (IC50 = 5.5 µM) in a reversible, non-competitive manner.

PTP Inhibitor XXXI, II-B08 - Calbiochem: SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.

Synonyme: CD45 Inhibitor V, FAP1 Inhibitor, LMWPTP Inhibitor, Lyp Inhibitor III, PTP1B Inhibitor IX, SHP1 Inhibitor IX, 3-(1-(3-(Biphenyl-4-ylamino)-3-oxopropyl)-1H-1,2,3-triazol-4-yl)-6-hydroxy-1-methyl-2-phenyl-1H-indole-5-carboxylic acid, SHP2 Inhibitor VI

Primary Target: SHP2
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      Übersicht

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₃₃H₂₇N₅O₄
      Description
      OverviewA cell-permeable indolo-salicylic acid compound that is shown to target SHP2 catalytic domain and inhibit SHP2-catalyzed pNPP hydrolysis (IC50 = 5.5 µM) in a reversible and non-competitive manner (Ki = 5.2 µM), exhibiting 2.6- to 5.7-fold selectivity over PTP1B, SHP1, FAP1, Lyp, CD45, and LMWPTP (IC50 = 14.3, 15.7, 20.3, 25.0, 30.0, and 31.1 µM, respectively). Effectively blocks SHP2-mediated human hematopoietic progenitor cell hyperproliferation (10 µM) due to SHP2 mutations (D61Y and E76K) or GM-CSF stimulation, as well as c-kit-dependent (due to D814V mutation or via ligand stimulation), SHP2-mediated myeloid proliferation (5 to 75 µM). Dual PI-3K and SHP2 inhibition by LY294002 (Cat. Nos. 440202 & 440204) and II-B08 (10 mg/kg and 50 mg/kg, respectively; daily i.p.) is shown to greatly prolong the survival rate of mice bearing D814V KIT-expressing 32D cells in vivo.
      Catalogue Number565852
      Brand Family Calbiochem®
      SynonymsCD45 Inhibitor V, FAP1 Inhibitor, LMWPTP Inhibitor, Lyp Inhibitor III, PTP1B Inhibitor IX, SHP1 Inhibitor IX, 3-(1-(3-(Biphenyl-4-ylamino)-3-oxopropyl)-1H-1,2,3-triazol-4-yl)-6-hydroxy-1-methyl-2-phenyl-1H-indole-5-carboxylic acid, SHP2 Inhibitor VI
      References
      ReferencesMali, R.S., et al. 2012. Blood 120, 2669.
      Zhang, X., et al. 2010. J. Med. Chem. 53, 2482.
      Product Information
      FormYellowish white powder
      Hill FormulaC₃₃H₂₇N₅O₄
      Chemical formulaC₃₃H₂₇N₅O₄
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ200
      Applications
      ApplicationPTP Inhibitor XXXI, II-B08, is a cell-permeable compound that targets SHP2 catalytic domain and inhibit SHP2-catalyzed pNPP hydrolysis (IC50 = 5.5 µM) in a reversible, non-competitive manner.
      Biological Information
      Primary TargetSHP2
      Primary Target IC<sub>50</sub>5.5, 9.0 and 10.8 µ
      Primary Target K<sub>i</sub>5.2 µ
      Secondary targetOther PTPs
      Purity≥98% 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 Ambient Temperature Only
      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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      565852 0

      Documentation

      PTP Inhibitor XXXI, II-B08 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      PTP Inhibitor XXXI, II-B08 - Calbiochem Analysenzertifikate

      TitelChargennummer
      565852

      Literatur

      Übersicht
      Mali, R.S., et al. 2012. Blood 120, 2669.
      Zhang, X., et al. 2010. J. Med. Chem. 53, 2482.
      Datenblatt

      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.

      Revision16-April-2013 JSW
      SynonymsCD45 Inhibitor V, FAP1 Inhibitor, LMWPTP Inhibitor, Lyp Inhibitor III, PTP1B Inhibitor IX, SHP1 Inhibitor IX, 3-(1-(3-(Biphenyl-4-ylamino)-3-oxopropyl)-1H-1,2,3-triazol-4-yl)-6-hydroxy-1-methyl-2-phenyl-1H-indole-5-carboxylic acid, SHP2 Inhibitor VI
      DescriptionA cell-permeable indolo-salicylic acid compound that is shown to target SHP2 catalytic domain and inhibit SHP2-catalyzed pNPP hydrolysis (IC50 = 5.5 µM) in a reversible and non-competitive manner (Ki = 5.2 µM), exhibiting 2.6- to 5.7-fold selectivity over PTP1B, SHP1, FAP1, Lyp, CD45, and LMWPTP (IC50 = 14.3, 15.7, 20.3, 25.0, 30.0, and 31.1 µM, respectively) and >9-fold selectivity over Cdc14A, HePTP, LAR, PTPα, and VHR (IC50 >50 µM). Effectively blocks hyperproliferative activity of human hematopoietic progenitor cells (Effective conc. = 10 µM) due to SHP2 mutations (D61Y and E76K) or GM-CSF stimulation, as well as c-kit-dependent (via ligand stimulation or D814V mutation), SHP2-mediated myeloid proliferation (Effective conc. = 5 to 75 µM). Dual PI-3K and SHP2 inhibition by LY294002 (Cat. Nos. 440202 & 440204) and II-B08 (10 mg/kg and 50 mg/kg, respectively; daily i.p.) is shown to greatly prolong the survival rate in a D814V KIT-expressing 32D-based murine MPD (myeloproliferative disease) model (0% survival rate on day 23, 27, 28, respectively, with DMSO, LY294002, II-B08 treatment alone; 20% survival rate on day 65 with combined treatment) in vivo.
      FormYellowish white powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₃₃H₂₇N₅O₄
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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
      ReferencesMali, R.S., et al. 2012. Blood 120, 2669.
      Zhang, X., et al. 2010. J. Med. Chem. 53, 2482.