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Art. -Nr.: HY-139150

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EZH2-IN-4

EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC₅₀s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2088132-99-2
Formel: C₂₉H₄₁N₃O₃S
Molecular Weight:511.72

Speicherung:

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

Data Sheet (269 KB)

EZH2-IN-4 Chemical Structure

CAS. Nr.: 2088132-99-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

WT 5-mer EZH2

0.923 nM (IC₅₀)

mut 5-mer EZH2

2.65 nM (IC₅₀)

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

In Vitro

EZH2-IN-4 (example 38) shows a cell H3K27me3 IC₅₀ of 0.00973 nM in Karpas-422 (EZH2 Y641N) cells^[1].
EZH2-IN-4 shows an IC₅₀ of 10.1 nM in Plate Kj«pas-422 cells^[1].
EZH2-IN-4 inhibits the proliferation of ovarian cancer cell lines (COV-434, TOV-21G, TOV-112D, A2780, Caov-3, OVCAR3; IC₅₀s=0.02-8.6 μM) and has no effect on SKOV3, HeyA8, HEC59 cell (IC₅₀>20 μM)^[1].

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

In Vivo

EZH2-IN-4 (example 38; oral gavage; 15 mpk; BID) results in 73% inhibition of tumor methylation in the Karpas-422 xenograft model^[1].
EZH2-IN-4 (po; 50 mpk; twice a day; pretreatment for 5 days; followed by co-administration with gemcitabine plus cisplatin for at least 23 additional days) significant inhibits A2780 tumor growth in A2780 xenograft model^[1].

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

Chemical Information

CAS. Nr. 2088132-99-2
Molecular Weight 511.72
Formel C₂₉H₄₁N₃O₃S
SMILES

CC1=C([C@@H]([C@@]2([H])CC[C@@](N3CC(C3)OC)([H])CC2)C)SC(CCCN4CC5=C(C=C(NC5=O)C)C)=C1C4=O
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

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Esteban DOMINGUEZ, et al. Inhibitors of ezh2. WO2017035060A1.

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.

100 mg

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