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528117 PI 3-K inhibitor IX, PIK-90 - CAS 677338-12-4 - Calbiochem

The PI 3-K inhibitor IX, PIK-90, also referenced under CAS 677338-12-4, controls the biological activity of PI 3-K. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: N-(2,3-Dihydro-7,8-dimethoxyimidazo[1,2-c]quinazolin-5-yl)-3-pyridinecarboxamide, mTOR Inhibitor VI

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528117
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Tableau de caractéristiques principal

CAS #Empirical Formula
677338-12-4C₁₈H₁₇N₅O₃

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528117-5MG
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      Description
      OverviewA cell-permeable imidazoquinazoline compound that acts as a potent, reversible, and ATP-competitive inhibitor against all three classes of PI 3-K kinases (IC50 = 11, 18, 47, 58, 64, 350, and 830 nM against p110α, p110γ, PI 3-KC2α, p110δ, PI 3-KC2β, p110β, and hsVPS34, respectively), as well as several PIKKs (IC50 = 13, 610, and 1050 nM against DNA-PK, ATM, and mTORC1, respectively) and PI 4-KIIIα (IC50 = 830 nM), while exhibiting much reduced potency against PI 4-KIIIβ and ATR (IC50 = 3.1 and 15 µM, respectively) and little or no activity toward PI 4-KIIα, PIPKs (IC50 >100 µM), and a panel of 36 commonly studied protein kinases (<15% inhibition at 10 µM). Effectively suppreses insulin-stimulated phosphorylations of Akt and rpS6 in 3T3-L1 adipocytes and L6 myotubes in a dose-dependent manner in vitro (by >90% at 2.5 µM) and completely prevents insulin-induced blood glucose decline in mice in vivo (10 mg/ml, i.p.).
      Catalogue Number528117
      Brand Family Calbiochem®
      SynonymsN-(2,3-Dihydro-7,8-dimethoxyimidazo[1,2-c]quinazolin-5-yl)-3-pyridinecarboxamide, mTOR Inhibitor VI
      References
      ReferencesFan, Q.W., et al. 2007. Cancer Res. 67, 7960.
      Fan, Q.W., et al. 2006. Cancer Cell 9, 341.
      Knight, Z.A., et al. 2006. Cell 125, 733.
      Product Information
      CAS number677338-12-4
      FormPale yellow solid
      Hill FormulaC₁₈H₁₇N₅O₃
      Chemical formulaC₁₈H₁₇N₅O₃
      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
      S PhraseS: 22-24/25

      Do not breathe dust.
      Avoid contact with skin and eyes.
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Blue Ice 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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      528117-5MG 04055977197006

      Documentation

      PI 3-K inhibitor IX, PIK-90 - CAS 677338-12-4 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      PI 3-K inhibitor IX, PIK-90 - CAS 677338-12-4 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      528117

      Références bibliographiques

      Aperçu de la référence bibliographique
      Fan, Q.W., et al. 2007. Cancer Res. 67, 7960.
      Fan, Q.W., et al. 2006. Cancer Cell 9, 341.
      Knight, Z.A., et al. 2006. Cell 125, 733.
      Fiche technique

      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.

      Revision10-February-2011 RFH
      SynonymsN-(2,3-Dihydro-7,8-dimethoxyimidazo[1,2-c]quinazolin-5-yl)-3-pyridinecarboxamide, mTOR Inhibitor VI
      DescriptionA cell-permeable imidazoquinazoline compound that acts as a potent, reversible, and ATP-competitive inhibitor against all three classes of PI 3-K kinases (IC50 = 11, 18, 47, 58, 64, 350, and 830 nM against p110α, p110γ, PI 3-KC2α, p110δ, PI 3-KC2β, p110β, and hsVPS34, respectively), as well as several PIKKs (IC50 = 13, 610, and 1050 nM against DNA-PK, ATM, and mTORC1, respectively) and PI 4-KIIIα (IC50 = 830 nM), while exhibiting much reduced potency against PI 4-KIIIβ and ATR (IC50 = 3.1 and 15 µM, respectively) and little or no activity toward PI 4-KIIα, PIPKs (IC50 >100 µM), and a panel of 36 commonly studied protein kinases (<15% inhibition at 10 µM). Effectively suppreses insulin-stimulated phosphorylations of Akt and rpS6 in 3T3-L1 adipocytes and L6 myotubes in a dose-dependent manner in vitro (by >90% at 2.5 µM) and completely prevents insulin-induced blood glucose decline in mice in vivo (10 mg/ml, i.p.).
      FormPale yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number677338-12-4
      Chemical formulaC₁₈H₁₇N₅O₃
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (0.5 mg/ml). Slight warming may be required to for complete solubility.
      Storage Protect from light
      -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesFan, Q.W., et al. 2007. Cancer Res. 67, 7960.
      Fan, Q.W., et al. 2006. Cancer Cell 9, 341.
      Knight, Z.A., et al. 2006. Cell 125, 733.