526528 | PIM-Kinase Inhibitor IX, SGI-1776 - Calbiochem

526528
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₀H₂₂F₃N₅O • 2H₂SO₄

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      526528-10MG
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      Stocked 
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          Glass bottle 10 mg
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          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
          FormOff-white powder
          Hill FormulaC₂₀H₂₂F₃N₅O • 2H₂SO₄
          Chemical formulaC₂₀H₂₂F₃N₅O • 2H₂SO₄
          Hygroscopic Hygroscopic
          Structure formula ImageStructure formula Image
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          526528

          References

          Reference overview
          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.
          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.

          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
          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 +2°C to +8°C
          Hygroscopic
          Protect from light
          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.