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

533936
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₈H₃₉N₇O₃ 755038-02-9

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      5.33936.0001
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          Glass bottle 10 mg
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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
          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.