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372040 Haspin Kinase Inhibitor, CHR-6494 - CAS 1333377-65-3 - Calbiochem

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Synonyme: 3-(1H-Indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine, Haploid Germ Cell-Specific Nuclear Protein Kinase Inhibitor, CHR-6494, Indazolyl-propylimidazopyridazin-amine

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372040
Preis & Verfügbarkeit

Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
1333377-65-3C₁₆H₁₆N₆

Preis & Verfügbarkeit

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372040-10MG
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      Description
      OverviewA cell-permeable indazolylimidazopyridazinamine compound that acts as a potent and reversible inhibitor of histone kinase haspin activity (IC50 = 2 nM) with moderate selectivity over TrkA, GSK-3β, PIM1, Cdk1/B and Cdk2/A (% inhibition at 100 nM = 58, 48, 36, 34 and 33, respectively) among a panel of 27-kinases. Shown to block pH3-Thr3, with no effect on pH3-Ser10 and pH3-Ser28, cause mitotic catastrophe, upregulate BUB1 and cyclin B1 levels, and potently induce apoptosis (IC50 = 473, 500 and 752 nM in HeLa, HCT-116 and MDA-MB-231 cells, respectively). Further, efficiently blocks bFGF-induced sprouting vessel by 70% at 1 µM (chicken embryo aortic arch ring assay) and suppresses tumor growth in HCT-116 xenografted mouse model (50 mg/kg, i.p.).
      Catalogue Number372040
      Brand Family Calbiochem®
      Synonyms3-(1H-Indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine, Haploid Germ Cell-Specific Nuclear Protein Kinase Inhibitor, CHR-6494, Indazolyl-propylimidazopyridazin-amine
      References
      ReferencesHuertas, D., et al. 2012. Oncogene 31, 1408.
      Product Information
      CAS number1333377-65-3
      FormOff-white solid
      Hill FormulaC₁₆H₁₆N₆
      Chemical formulaC₁₆H₁₆N₆
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliqout 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
      372040-10MG 04055977213553

      Documentation

      Haspin Kinase Inhibitor, CHR-6494 - CAS 1333377-65-3 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Haspin Kinase Inhibitor, CHR-6494 - CAS 1333377-65-3 - Calbiochem Analysenzertifikate

      TitelChargennummer
      372040

      Literatur

      Übersicht
      Huertas, D., et al. 2012. Oncogene 31, 1408.
      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.

      Revision06-February-2013 JSW
      Synonyms3-(1H-Indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine, Haploid Germ Cell-Specific Nuclear Protein Kinase Inhibitor, CHR-6494, Indazolyl-propylimidazopyridazin-amine
      DescriptionA cell-permeable indazolylimidazopyridazinamine compound that acts as a potent and reversible inhibitor of histone kinase haspin activity (IC50 = 2 nM) with moderate selectivity over TrkA, GSK-3β, PIM1, Cdk1/B and Cdk2/A (% inhibition at 100 nM = 58, 48, 36, 34 and 33, respectively) among a panel of 27-kinases. Shown to block pH3-Thr3, with no effect on pH3-Ser10 and pH3-Ser28, cause mitotic catastrophe, upregulate BUB1 and cyclin B1 levels, and potently induce apoptosis (IC50 = 473, 500 and 752 nM in HeLa, HCT-116 and MDA-MB-231 cells, respectively). Further, efficiently blocks bFGF-induced sprouting vessel by 70% at 1 µM (chicken embryo aortic arch ring assay) and suppresses tumor growth in HCT-116 xenografted mouse model (50 mg/kg, i.p.).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1333377-65-3
      Chemical formulaC₁₆H₁₆N₆
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (25 mg/ml)
      Storage Protect from light
      -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliqout and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesHuertas, D., et al. 2012. Oncogene 31, 1408.