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533936 Polo-like Kinase Inhibitor IV, BI 2536 - CAS 755038-02-9 - Calbiochem

533936
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Key Specifications Table

Empirical FormulaCAS #
C₂₈H₃₉N₇O₃ 755038-02-9

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      Description
      OverviewA cell-permeable, bioavailable, non-toxic dihydropteridinone derived compound that acts as a highly potent, selective, reversible, and ATP-competitive inhibitor of polo-like kinase 1 (PLK1; IC50 = 830 pM). At higher concentrations it is shown to block the activity of PLK2 (IC50 = 3.5 nM) and PLK3 (IC50 = 9.0 nM). Displays equipotency against human, rat, and mouse PLK1 and does not affect the activity of 63 other protein kinases studied. Demonstrates greater selectivity for cancer cells and has much reduced effect on non-transformed cells. Has high affinity for bromodomain 4 (BRD4; Kd = 37 nM) and displace it from chromatin and down-regulates the expression of c-Myc in MM.1S multiple myeloma cells. Blocks PLK1 enrichment at kinetochores and centrosomes. Induces cell cycle arrest at G2/M phase leading to apoptosis. Shown to arrest the proliferation of 32 different cancer cell lines (EC50 = 2 - 25 nM) exhibiting varied patterns of oncogenic or tumor suppressor mutations and completely suppresses the growth of HCT116 colon cancer xenografts in nude mice (40-50 mg/kg, i.v., once or twice/week).

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533936
      Brand Family Calbiochem®
      SynonymsBI-2536, 4-((R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-ylamino)-3-methoxy-N-(1-methyl-piperidin-4-yl)-benzamide, PlK1 Inhibitor IV, BRD4 Inhibitor VII
      References
      ReferencesCiceri, P., et al. 2014. Nat. Chem. Biol. 10, 305.
      Nappi, T.C., et al. 2009. Cancer Res. 69, 1916.
      Steegmaier M, et al. 2007. Curr. Biol. 17, 316.
      Lenart, P., et al. 2007. Curr. Biol. 17, 304.
      Product Information
      CAS number755038-02-9
      FormLight yellow solid
      Hill FormulaC₂₈H₃₉N₇O₃
      Chemical formulaC₂₈H₃₉N₇O₃
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPLK1
      Primary Target IC<sub>50</sub>830 pM for PLK1
      Secondary targetBRD4
      Purity≥98% 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 Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°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

      Documentation

      Polo-like Kinase Inhibitor IV, BI 2536 - CAS 755038-02-9 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Ciceri, P., et al. 2014. Nat. Chem. Biol. 10, 305.
      Nappi, T.C., et al. 2009. Cancer Res. 69, 1916.
      Steegmaier M, et al. 2007. Curr. Biol. 17, 316.
      Lenart, P., et al. 2007. Curr. Biol. 17, 304.
      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.

      Revision20-November-2015 JSW
      SynonymsBI-2536, 4-((R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-ylamino)-3-methoxy-N-(1-methyl-piperidin-4-yl)-benzamide, PlK1 Inhibitor IV, BRD4 Inhibitor VII
      DescriptionA cell-permeable, bioavailable, non-toxic dihydropteridinone derived compound that acts as a highly potent, selective, reversible, and ATP-competitive inhibitor of polo-like kinase 1 (PLK1; IC50 = 830 pM). At higher concentrations it is shown to block the activity of PLK2 (IC50 = 3.5 nM) and PLK3 (IC50 = 9.0 nM). Displays equipotency against human, rat, and mouse PLK1 and does not affect the activity of 63 other protein kinases studied. Demonstrates greater selectivity for cancer cells and has much reduced effect on non-transformed cells. Has high affinity for bromodomain 4 (BRD4; Kd = 37 nM) and displace it from chromatin and down-regulates the expression of c-Myc in MM.1S multiple myeloma cells. Blocks PLK1 enrichment at kinetochores and centrosomes. Induces cell cycle arrest at G2/M phase leading to apoptosis. Shown to arrest the proliferation of 32 different cancer cell lines (EC50 = 2 - 25 nM) exhibiting varied patterns of oncogenic or tumor suppressor mutations and completely suppresses the growth of HCT116 colon cancer xenografts in nude mice (40-50 mg/kg, i.v., once or twice/week).
      FormLight yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number755038-02-9
      Chemical formulaC₂₈H₃₉N₇O₃
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage +2°C to +8°C
      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
      ReferencesCiceri, P., et al. 2014. Nat. Chem. Biol. 10, 305.
      Nappi, T.C., et al. 2009. Cancer Res. 69, 1916.
      Steegmaier M, et al. 2007. Curr. Biol. 17, 316.
      Lenart, P., et al. 2007. Curr. Biol. 17, 304.