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Art. -Nr.: HY-118447

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RO0505124

RO0505124 is a selective CDK4 inhibitor with an IC₅₀ of 20 nM. RO0505124 reversibly binds the ATP pocket of the kinase. RO0505124 induces G1 phase arrest in cancer cells via reduced retinoblastoma protein (Rb) phosphorylation, blocking S phase progression. RO0505124 exhibits anti-proliferative activity against various cancer cells. RO0505124 delays mitosis, induces aberrant mitosis with lagging chromosomes, driving mitotic slippage and formation of multinucleated or micronucleated cells. RO0505124 inhibits G2/M phase accumulation of survivin and borealin. RO0505124 can be used for the research of cancer.

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CAS. Nr.: 443913-79-9
Formel: C₂₃H₂₅N₅O₃S
Molecular Weight:451.55

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

RO0505124 Chemical Structure

CAS. Nr.: 443913-79-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CDK4

20 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
COLO 205	IC₅₀	2.04 μM Compound: Ro-0505124	Antiproliferative activity against human COLO205 cells assessed as inhibition of S phase after 48 hrs by MTT assay Antiproliferative activity against human COLO205 cells assessed as inhibition of S phase after 48 hrs by MTT assay	[PMID: 16476733]
HCT-116	IC₅₀	3.85 μM Compound: Ro-0505124	Antiproliferative activity against human HCT116 cells assessed as inhibition of S phase after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as inhibition of S phase after 48 hrs by MTT assay	[PMID: 16476733]
HCT-116	IC₅₀	3.9 μM Compound: Ro-0505124	Cell cycle arrest in Rb-competent human HCT116 cells assessed as reduction in S phase after 24 hrs using BrdUrd staining by FACS analysis Cell cycle arrest in Rb-competent human HCT116 cells assessed as reduction in S phase after 24 hrs using BrdUrd staining by FACS analysis	[PMID: 16476733]
MDA-MB-435	IC₅₀	3.06 μM Compound: Ro-0505124	Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of S phase after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of S phase after 48 hrs by MTT assay	[PMID: 16476733]
MDA-MB-453	IC₅₀	1.45 μM Compound: Ro-0505124	Antiproliferative activity against human MDA-MB-453 assessed as inhibition of S phase cells after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-453 assessed as inhibition of S phase cells after 48 hrs by MTT assay	[PMID: 16476733]
NCI-H460	IC₅₀	8.12 μM Compound: Ro-0505124	Antiproliferative activity against human H460a cells assessed as inhibition of S phase after 48 hrs by MTT assay Antiproliferative activity against human H460a cells assessed as inhibition of S phase after 48 hrs by MTT assay	[PMID: 16476733]
RKO	IC₅₀	1.6 μM Compound: Ro-0505124	Antiproliferative activity against human RKO cells assessed as inhibition of S phase after 48 hrs by MTT assay Antiproliferative activity against human RKO cells assessed as inhibition of S phase after 48 hrs by MTT assay	[PMID: 16476733]
SW480	IC₅₀	3.67 μM Compound: Ro-0505124	Antiproliferative activity against human SW480 cells assessed as inhibition of S phase after 48 hrs by MTT assay Antiproliferative activity against human SW480 cells assessed as inhibition of S phase after 48 hrs by MTT assay	[PMID: 16476733]

In Vitro

RO0505124 (30 min) potently and selectively inhibits recombinant human CDK4-cyclin D with an IC₅₀ of 20 nM, showing >100-fold selectivity over CDK1 and CDK2, and relatively high selectivity across a panel of 128 kinases^[1].
RO0505124 (48 h) inhibits proliferation of multiple human cancer cell lines with IC₅₀ values ranging from 1.45 μM to 8.12 μM after 48 h of treatment^[1].
RO0505124 (3.9-18.3 μM; 4-24 h) induces a G₁ phase arrest and inhibits Rb phosphorylation in asynchronous HCT-116 cells^[1].
RO0505124 (2 μM; 0-24 h) delays mitotic entry, prolongs mitotic duration, and induces aberrant mitosis^[1].
RO0505124 (2 μM; 3-14 h) delays the accumulation of survivin and borealin proteins during G₂/M phase in HeLa cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

asynchronous HCT-116 cells
Concentration:

3.9, 6.1, 18.3 μM
Incubation Time:

4, 24 h
Result:

Reduced S phase to 50% of control levels and significantly decreased Rb phosphorylation at the IC₅₀ concentration of 3.9 μM.
Further inhibited BrdUrd incorporation and Rb phosphorylation at higher doses.
Caused a G₁ phase arrest with no reduction in G₂/M phase cell proportion at higher doses.

Chemical Information

CAS. Nr. 443913-79-9
Molecular Weight 451.55
Formel C₂₃H₂₅N₅O₃S
SMILES

O=C(C1=CC=C2OCCOC2=C1)C=3SC(=NC3N)NC4=CC=C(C=C4)N5CCN(C)CC5
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Burgess A, et al. Inhibition of S/G2 phase CDK4 reduces mitotic fidelity[J]. Journal of Biological Chemistry, 2006, 281(15): 9987-9995. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
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RO0505124

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

RO0505124 Related Classifications

HY-118447 Related Classifications