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

530487
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Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₂₄H₂₉N₇O₂ • HCl 827022-32-2

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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
      Quality LevelMQ100
      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.