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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 applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Replacement Information

Key Spec Table

CAS #Empirical Formula
546102-60-7C₂₀H₁₀BrN₃O₂

Products

Catalogue NumberPackaging Qty/Pack
219476-1MG Plastic ampoule 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
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
Global Trade Item Number
Catalogue Number GTIN
219476-1MG 04055977218534

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 Protect from light
+2°C to +8°C
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.