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513028 PD 166285 - CAS 212391-63-4 - Calbiochem

A cell-permeable, orally bioavailable, ATP-competitive, broad-spectrum tyrosine kinase inhibitor that suppresses angiogenesis both in vitro and in vivo.

PD 166285 - CAS 212391-63-4 - Calbiochem : FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: PD166285, PD0166285, 6-(2,6-Dichlorophenyl)-2-(4-(2-(diethylaminoethoxy)-phenylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one, 2HCl, Wee1 Inhibitor IV, PDGFR Tyrosine Kinase Inhibitor XIX

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      Aperçu

      Replacement Information

      Tableau de caractéristiques principal

      CAS #Empirical Formula
      212391-63-4C₂₆H₂₇Cl₂N₅O₂ • 2HCl
      Description
      OverviewA cell-permeable, orally bioavailable, ATP-competitive, broad-spectrum tyrosine kinase inhibitor (IC50 against against c-Src, Wee1, FGFR-1, Myt1, EGFR, and PDGFRβ = 8.4, 24, 39.3, 72, 87.5 and 98.3 nM, respectively) that suppresses angiogenesis both in vitro (max inhibition dose at 100 nM in HUVEC microcapillary formation assays) and in vivo (max inhibition achieved via 5 mg/kg p.o. in murine Matrigel plug angiogenesis assays), while exhibiting much reduced potency against Chk1, MAPK, and PKC (IC50 = 3.4, 5, and 22.7 µM, respectively) and little activity toward IRTK and Cdk4/D1 even at concentrations as high as 50 µM. Shown to effectively block PDGF-, EGF-, and bFGF-stimulated receptor phosphorylations (IC50 = 6.5, 1600, and 97.3 nM, respectively) and other cellular responses in rat aortic smooth muscle cells. Inhibition of cellular Wee1 activity by 500 nM PD 166285 in combination with 50 ng/ml nocodazole (Cat. No. 487928) treatment is also reported to result in a blockage of radiation-induced Cdc2 phosphorylation on Tyr15 and Thr14 in 7 human cancer cells and specifically demonstrated to sensatize PA-1 cultures to radiation-induced cell death in a p53-dependent manner.
      Catalogue Number513028
      Brand Family Calbiochem®
      SynonymsPD166285, PD0166285, 6-(2,6-Dichlorophenyl)-2-(4-(2-(diethylaminoethoxy)-phenylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one, 2HCl, Wee1 Inhibitor IV, PDGFR Tyrosine Kinase Inhibitor XIX
      References
      ReferencesWang, Y., et al. 2001. Cancer Res. 61, 8211.
      Dimitroff, C.J., et al. 1999. Invest. New Drugs 17, 121.
      Roginskaya, V., et al. 1999. Leukemia 13, 855.
      Panek, R.L., et al. 1997. J. Pharmacol. Exp. Ther. 283, 1433.
      Product Information
      CAS number212391-63-4
      FormPale yellow solid
      Hill FormulaC₂₆H₂₇Cl₂N₅O₂ • 2HCl
      Chemical formulaC₂₆H₂₇Cl₂N₅O₂ • 2HCl
      Hygroscopic Hygroscopic
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥97% 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 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
      513028 0

      Documentation

      PD 166285 - CAS 212391-63-4 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      PD 166285 - CAS 212391-63-4 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      513028

      Références bibliographiques

      Aperçu de la référence bibliographique
      Wang, Y., et al. 2001. Cancer Res. 61, 8211.
      Dimitroff, C.J., et al. 1999. Invest. New Drugs 17, 121.
      Roginskaya, V., et al. 1999. Leukemia 13, 855.
      Panek, R.L., et al. 1997. J. Pharmacol. Exp. Ther. 283, 1433.
      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.

      Revision04-May-2011 RFH
      SynonymsPD166285, PD0166285, 6-(2,6-Dichlorophenyl)-2-(4-(2-(diethylaminoethoxy)-phenylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one, 2HCl, Wee1 Inhibitor IV, PDGFR Tyrosine Kinase Inhibitor XIX
      DescriptionA cell-permeable, orally bioavailable, ATP-competitive, broad-spectrum tyrosine kinase inhibitor (IC50 against against c-Src, Wee1, FGFR-1, Myt1, EGFR, and PDGFRβ = 8.4, 24, 39.3, 72, 87.5 and 98.3 nM, respectively) that suppresses angiogenesis both in vitro (max inhibition dose at 100 nM in HUVEC microcapillary formation assays) and in vivo (max inhibition achieved via 5 mg/kg p.o. in murine Matrigel plug angiogenesis assays), while exhibiting much reduced potency against Chk1, MAPK, and PKC (IC50 = 3.4, 5, and 22.7 µM, respectively) and little activity toward IRTK and Cdk4/D1 even at concentrations as high as 50 µM. Shown to effectively block PDGF-, EGF-, and bFGF-stimulated receptor phosphorylations (IC50 = 6.5, 1600, and 97.3 nM, respectively) and other cellular responses in rat aortic smooth muscle cells. Inhibition of cellular Wee1 activity by 500 nM PD 166285 in combination with 50 ng/ml nocodazole (Cat. No. 487928) treatment is also reported to result in a blockage of radiation-induced Cdc2 phosphorylation on Tyr15 and Thr14 in 7 human cancer cells and specifically demonstrated to sensatize PA-1 cultures to radiation-induced cell death in a p53-dependent manner.
      FormPale yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number212391-63-4
      Chemical formulaC₂₆H₂₇Cl₂N₅O₂ • 2HCl
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Hygroscopic
      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
      ReferencesWang, Y., et al. 2001. Cancer Res. 61, 8211.
      Dimitroff, C.J., et al. 1999. Invest. New Drugs 17, 121.
      Roginskaya, V., et al. 1999. Leukemia 13, 855.
      Panek, R.L., et al. 1997. J. Pharmacol. Exp. Ther. 283, 1433.