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

219476
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Overview

Key Spec Table

CAS #Empirical Formula
546102-60-7C₂₀H₁₀BrN₃O₂

Products

Catalogue NumberPackaging Qty/Pack
219476-1MGCN 塑膠安瓿;塑膠針藥瓶 1 mg
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
219476-1MGCN 04055977218534