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

513028
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₆H₂₇Cl₂N₅O₂ • 2HCl 212391-63-4

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      513028-5MG
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          5 mg
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          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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          513028

          References

          Reference overview
          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.
          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.

          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 +2°C to +8°C
          Hygroscopic
          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.
          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.