219476 Cdk4 Inhibitor - CAS 546102-60-7 - Calbiochem

219476
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Overview

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Key Specifications Table

Empirical FormulaCAS #
C₂₀H₁₀BrN₃O₂ 546102-60-7

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219476-1MG
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      Description
      OverviewA cell-permeable, unsymmetrical indolocarbazole compound that displays antiproliferative properties. Acts as a potent, selective, reversible and ATP-competitive inhibitor of Cdk4/D1 (IC50 = 76 nM). It inhibits the activity of other Cdk’s only at much higher concentrations (IC50 = 520 nM and 2.1 µM for Cdk2/E and Cdk1/B, respectively) and shows little activity towards CaMKII, PKA, or GSK-3β (IC50 ≥ 12.4 µM). Shown to inhibit tumor cells growth (IC50 < 3.0 µM in HCT-116 and NCI-H460 cells) by blocking Rb phosphorylation and inducing G1 cell cycle arrest.
      Catalogue Number219476
      Brand Family Calbiochem®
      Synonyms2-Bromo-12,13-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione
      References
      ReferencesZhu, G., et al. 2003. J. Med. Chem. 46, 2027.
      Product Information
      CAS number546102-60-7
      ATP CompetitiveY
      FormYellow solid
      Hill FormulaC₂₀H₁₀BrN₃O₂
      Chemical formulaC₂₀H₁₀BrN₃O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetCDK4/D1
      Primary Target IC<sub>50</sub>76 nM against Cdk4/D1; < 3.0 7micro;M inhibiting tumor cells growth in HCT-116 and NCI-H460 cells
      Purity≥95% 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 Carcinogenic / Teratogenic
      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

      Cdk4 Inhibitor - CAS 546102-60-7 - Calbiochem Certificates of Analysis

      TitleLot Number
      219476

      References

      Reference overview
      Zhu, G., et al. 2003. J. Med. Chem. 46, 2027.
      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.

      Revision29-December-2009 RFH
      Synonyms2-Bromo-12,13-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione
      DescriptionA cell-permeable, unsymmetrical indolocarbazole compound that displays antiproliferative properties. Acts as a potent, selective, reversible and ATP-competitive inhibitor of Cdk4/D1 (IC50 = 76 nM). It inhibits the activity of other Cdk’s only at much higher concentrations (IC50 = 520 nM and 2.1 µM for Cdk2/E and Cdk1/B, respectively) and shows little activity towards CaMKII, PKA, or GSK-3β (IC50 ≥ 12.4 µM). Shown to inhibit tumor cells growth (IC50 < 3.0 µM in HCT-116 and NCI-H460 cells) by blocking Rb phosphorylation and inducing G1 cell cycle arrest.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number546102-60-7
      Chemical formulaC₂₀H₁₀BrN₃O₂
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (1 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 Carcinogenic / Teratogenic
      ReferencesZhu, G., et al. 2003. J. Med. Chem. 46, 2027.