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

The Cdk4 Inhibitor, also referenced under CAS 546102-60-7, controls the biological activity of Cdk4. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applica

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Synonyms: 2-Bromo-12,13-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione

Primary Target: CDK4/D1
219476
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Overview

Key Spec Table

CAS #Empirical Formula
546102-60-7C₂₀H₁₀BrN₃O₂

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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
      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
      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
      Global Trade Item Number
      Catalogue Number GTIN
      219476-1MG 04055977218534