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526528 PIM-Kinase Inhibitor IX, SGI-1776 - CAS 1173928-26-1 - Calbiochem

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      Übersicht

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      1173928-26-1C₂₀H₂₂F₃N₅O • 2H₂SO₄
      Description
      OverviewA cell-permeable imidazopyridazine compound that acts as a potent, reversible and ATP-competitive inhibitor of Pim-1,2,3, Flt-3 and haspin kinase activities (IC50 = 7, 363, 69, 44 and 34 nM, respectively) with moderate (40% inhibition at 1 µM for c-kit) to excellent selectivity over CDKs, Aurora, Chk1, IKK, JNK, Abl, Raf, PKA, PKC and PI 3-K among 300-kinases. Shown to inhibit RNA synthesis, block phosphorylation of c-Myc-Ser62 and STAT3-Tyr705, and decrease c-Myc and Mcl-1 protein levels; cause cell cycle arrest and induce apoptosis in CLL lymphocytes and in AML cells, and efficiently arrest the growth of several prostate cancer cells (IC50 <10 µM).
      Catalogue Number526528
      Brand Family Calbiochem®
      SynonymsN-((1-Methylpiperidin-4-yl)methyl)-3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-amine, 2H₂SO₄
      References
      ReferencesChen, L.S., et al. 2011. Blood 118, 693.
      Chang, M., et al. 2010. Mol. Cancer Ther. 9, 2478.
      Mumenthaler, S.M., et al. 2009. Mol. Cancer Ther. 8, 2882.
      Chen, L.S., et al. 2009. Blood 114, 4150.
      Product Information
      CAS number1173928-26-1
      FormOff-white powder
      Hill FormulaC₂₀H₂₂F₃N₅O • 2H₂SO₄
      Chemical formulaC₂₀H₂₂F₃N₅O • 2H₂SO₄
      Hygroscopic Hygroscopic
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥99% 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
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstituion, 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
      526528 0

      Documentation

      PIM-Kinase Inhibitor IX, SGI-1776 - CAS 1173928-26-1 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      PIM-Kinase Inhibitor IX, SGI-1776 - CAS 1173928-26-1 - Calbiochem Analysenzertifikate

      TitelChargennummer
      526528

      Literatur

      Übersicht
      Chen, L.S., et al. 2011. Blood 118, 693.
      Chang, M., et al. 2010. Mol. Cancer Ther. 9, 2478.
      Mumenthaler, S.M., et al. 2009. Mol. Cancer Ther. 8, 2882.
      Chen, L.S., et al. 2009. Blood 114, 4150.
      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.

      Revision09-July-2012 JSW
      SynonymsN-((1-Methylpiperidin-4-yl)methyl)-3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-amine, 2H₂SO₄
      DescriptionA cell-permeable imidazopyridazine compound that acts as a potent, reversible and ATP-competitive inhibitor of Pim-1,2,3, Flt-3 and haspin kinase activities (IC50 = 7, 363, 69, 44 and 34 nM, respectively) with moderate (40% inhibition at 1 µM for c-kit) to excellent selectivity over CDKs, Aurora, Chk1, IKK, JNK, Abl, Raf, PKA, PKC and PI 3-K among 300-kinases. Shown to inhibit RNA synthesis, block phosphorylation of c-Myc-Ser62 and STAT3-Tyr705, and decrease c-Myc and Mcl-1 protein levels; cause cell cycle arrest and induce apoptosis in CLL lymphocytes and in AML cells, and efficiently arrest the growth of several prostate cancer cells (IC50 <10 µM).
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1173928-26-1
      Chemical formulaC₂₀H₂₂F₃N₅O • 2H₂SO₄
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (100 mg/ml; clear, nearly colorless solution) or H₂O (100 mg/ml; clear, nearly colorless solution)
      Storage Protect from light
      +2°C to +8°C
      Hygroscopic
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstituion, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesChen, L.S., et al. 2011. Blood 118, 693.
      Chang, M., et al. 2010. Mol. Cancer Ther. 9, 2478.
      Mumenthaler, S.M., et al. 2009. Mol. Cancer Ther. 8, 2882.
      Chen, L.S., et al. 2009. Blood 114, 4150.