530487 StemSelect® PD 0332991 - CAS 827022-32-2 - Calbiochem

530487
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₄H₂₉N₇O₂ • HCl 827022-32-2

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      5.30487.0001
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          Glass bottle 5 mg
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          Description
          OverviewA cell-permeable, orally available and brain permeant, non-toxic pyridopyrimidinone compound that acts as a potent, selective, reversible, ATP competitive inhibitor of Cdk4 and Cdk6 (IC50 = 11, 9, and 15 nM for Cdk4/D1, Cdk4/D3 and Cdk6/D2, respectively). Hence, it reduces retinoblastoma protein phosphorylation at Ser780/Ser795 (IC50 = 66 nM in MDA-435 cells) and arrests cell cycle at G1 phase. Acts as a cytostatic agent, but does induce apoptotic cell death when used alone. However, it potentiates the cytotoxicity of dexamethasone (Cat. No. 265005), bortezomib (Cat. No. 504314), and tamoxifen (Cat. No. 579000) in estrogen receptor (ER)-positive cell lines. Exhibits only a trivial inhibitory activity towards Cdk2/E2, Cdk2/A, Cdk1/B and Cdk5/p25 in a 36-kinase panel (IC50 > 10 µM). Improves endoderm differentiation of late G1-human embryonic stem cells expressing Smad2 or Smad3 (~ 750 nM) and further enhances endoderm differentiation into hepatic and pancreatic progenitor cells. Shown to regress the growth of human breast tumor xenografts in murine models (~150 mg/kg, p.o., daily).

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number530487
          Brand Family Calbiochem®
          Synonyms6-Acetyl-8-cyclopentyl-5-methyl-2-(5-(piperazin-1-yl)pyridin-2-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one, HCl, Cdk4/Cdk6 Inhibitor V, PD-0332991, HCl, PF-332991, HCl
          References
          ReferencesPauklin, S. and Vallier, L., 2013. Cell 155, 135.
          Finn, R.S., et al. 2009. Breast Cancer Res. 11, R17.
          Menu, E., et al. 2008. Cancer Res. 68, 5519.
          Baughn, L.B., et al. 2006. Cancer Res. 66, 7661.
          Fry, D.W., et al. 2004. Mol. Cancer Ther. 3, 1427.
          Product Information
          CAS number827022-32-2
          FormYellow liquid
          Hill FormulaC₂₄H₂₉N₇O₂ • HCl
          Chemical formulaC₂₄H₂₉N₇O₂ • HCl
          ReversibleY
          Applications
          Biological Information
          Primary TargetCdk4 & Cdk6
          Purity≥97% by HPLC
          Physicochemical Information
          Cell permeableY
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Dry Ice Only
          Toxicity Standard Handling
          Storage ≤ -70°C
          Protect from Light Protect from light
          Avoid freeze/thaw Avoid freeze/thaw
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, 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

          StemSelect® PD 0332991 - CAS 827022-32-2 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Pauklin, S. and Vallier, L., 2013. Cell 155, 135.
          Finn, R.S., et al. 2009. Breast Cancer Res. 11, R17.
          Menu, E., et al. 2008. Cancer Res. 68, 5519.
          Baughn, L.B., et al. 2006. Cancer Res. 66, 7661.
          Fry, D.W., et al. 2004. Mol. Cancer Ther. 3, 1427.
          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.

          Revision02-May-2014 JSW
          Synonyms6-Acetyl-8-cyclopentyl-5-methyl-2-(5-(piperazin-1-yl)pyridin-2-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one, HCl, Cdk4/Cdk6 Inhibitor V, PD-0332991, HCl, PF-332991, HCl
          DescriptionA cell-permeable, orally available and brain permeant, non-toxic pyridopyrimidinone compound that acts as a potent, selective, reversible, ATP competitive inhibitor of Cdk4 and Cdk6 (IC50 = 11, 9, and 15 nM for Cdk4/D1, Cdk4/D3 and Cdk6/D2, respectively). Hence, it reduces retinoblastoma protein phosphorylation at Ser780/Ser795 (IC50 = 66 nM in MDA-435 cells) and arrests cell cycle at G1 phase. Acts as a cytostatic agent, but does induce apoptotic cell death when used alone. However, it potentiates the cytotoxicity of dexamethasone (Cat. No. 265005), bortezomib (Cat. No. 504314), and tamoxifen (Cat. No. 579000) in estrogen receptor (ER)-positive cell lines. Exhibits only a trivial inhibitory activity towards Cdk2/E2, Cdk2/A, Cdk1/B and Cdk5/p25 in a 36-kinase panel (IC50 > 10 µM). Improves endoderm differentiation of late G1-human embryonic stem cells expressing Smad2 or Smad3 (~ 750 nM) and further enhances endoderm differentiation into hepatic and pancreatic progenitor cells. Shown to regress the growth of human breast tumor xenografts in murine models (~150 mg/kg, p.o., daily).
          FormYellow liquid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number827022-32-2
          Chemical formulaC₂₄H₂₉N₇O₂ • HCl
          Purity≥97% by HPLC
          SolubilityH₂O (10 mg/ml)
          Storage ≤ -70°C
          Protect from light
          Avoid freeze/thaw
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesPauklin, S. and Vallier, L., 2013. Cell 155, 135.
          Finn, R.S., et al. 2009. Breast Cancer Res. 11, R17.
          Menu, E., et al. 2008. Cancer Res. 68, 5519.
          Baughn, L.B., et al. 2006. Cancer Res. 66, 7661.
          Fry, D.W., et al. 2004. Mol. Cancer Ther. 3, 1427.