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Art. -Nr.: HY-146999

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YM458

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YM458 is a potent EZH2 and BRD4 dual inhibitor with IC₅₀s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer.

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Reinheit: 99.16%
CAS. Nr.: 2770108-93-3
Formel: C₅₃H₆₁ClN₈O₅S
Molecular Weight:957.62

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

YM458 Chemical Structure

CAS. Nr.: 2770108-93-3

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Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

EZH2

490 nM (IC₅₀)

BRD4

34 nM (IC₅₀)

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
ASPC1	IC₅₀	0.69 μM Compound: 27	Antiproliferative activity against human ASPC1 cells harboring KRAS G12D mutant assessed as reduction in cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human ASPC1 cells harboring KRAS G12D mutant assessed as reduction in cell growth measured after 72 hrs by MTT assay	[PMID: 37156182]
ASPC1	IC₅₀	0.69 μM Compound: D7; YM458	Antiproliferative activity against human ASPC1 cells assessed as cell growth inhibition incubated for 6 days by MTS assay Antiproliferative activity against human ASPC1 cells assessed as cell growth inhibition incubated for 6 days by MTS assay	[PMID: 35500243]

In Vitro

YM458 (compound D7) (0-30 μM; 6 days) has antiproliferative activities against AsPC-1 cells with an IC₅₀ of 0.69 ± 0.16 μM; and (1 μM; 72 hours) significantly decreases the degree of H3K27me3 and c-Myc in AsPC-1^[1].
YM458 (0-30 μM; 4 or 6 days) inhibits cell proliferation on a broad range of solid cancer cells, and significantly suppresses proliferation of A549 lung cancer cells and HCT116 colorectal cancer cells at 1 μM^[1].
YM458 (0.05-0.4 μM; 12-20 days) inhibits colony formation of AsPC-1, HCT116, and A549 cancer cells in a dose-dependent manner^[1].

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

Western Blot Analysis

Cell Line:

AsPC-1^[1]
Concentration:

1 μM
Incubation Time:

72 hours
Result:

Decreased the degree of H3K27me3 and c-Myc significantly.

Cell Proliferation Assay

Cell Line:

AsPC-1, SW1990, CFPAC-1, A549, HCC827, H1650, H292, H460, DLD1, HCT116, and RKO^[1]
Concentration:

0-30 μM
Incubation Time:

4 or 6 days
Result:

Inhibited cell proliferation on a broad range of solid cancer cells, and significantly suppressed proliferation of A549 lung cancer cells and HCT116 colorectal cancer cells at 1 μM.

In Vivo

YM458 (60 mg/kg; IP; every other day, for 38 days) prevents tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells^[1].
Pharmacokinetic Parameters of YM458 in Female BALB/c mice^[1].

	IP (80 mg/kg)	PO (80 mg/kg)
t_1/2 (h)	3.81	4.16
T_max (h)	1	1
C_max (ng/mL)	27126.3	4383.6
AUC_0-24 (ng/mL·h)	273220.1	13509.1
CL (mL/min/kg)	4.88
F (%)		4.94

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

Animal Model:

BALB/c nude mice (injected with A549 or AsPC-1)^[1]
Dosage:

60 mg/kg
Administration:

IP; every other day, for 38 days
Result:

Prevented tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells.

Chemical Information

CAS. Nr. 2770108-93-3
Appearance Solid
Molecular Weight 957.62
Formel C₅₃H₆₁ClN₈O₅S
Color White to off-white
SMILES

CC1=C(C)SC2=C1C(C3=CC=C(C=C3)Cl)=N[C@@H](CC(NCCCCCOC4=CC=C(C5=CC(N(C6CCOCC6)CC)=C(C(C(NCC7=C(C=C(NC7=O)C)C)=O)=C5)C)C=C4)=O)C8=NN=C(C)N28
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (130.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.0443 mL

5.2213 mL

10.4426 mL

5 mM

0.2089 mL

1.0443 mL

2.0885 mL

10 mM

0.1044 mL

0.5221 mL

1.0443 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Guo Z, et al. Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors. J Med Chem. 2022;65(9):6573-6592. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.0443 mL	5.2213 mL	10.4426 mL	26.1064 mL
	5 mM	0.2089 mL	1.0443 mL	2.0885 mL	5.2213 mL
	10 mM	0.1044 mL	0.5221 mL	1.0443 mL	2.6106 mL
	15 mM	0.0696 mL	0.3481 mL	0.6962 mL	1.7404 mL
	20 mM	0.0522 mL	0.2611 mL	0.5221 mL	1.3053 mL
	25 mM	0.0418 mL	0.2089 mL	0.4177 mL	1.0443 mL
	30 mM	0.0348 mL	0.1740 mL	0.3481 mL	0.8702 mL
	40 mM	0.0261 mL	0.1305 mL	0.2611 mL	0.6527 mL
	50 mM	0.0209 mL	0.1044 mL	0.2089 mL	0.5221 mL
	60 mM	0.0174 mL	0.0870 mL	0.1740 mL	0.4351 mL
	80 mM	0.0131 mL	0.0653 mL	0.1305 mL	0.3263 mL
	100 mM	0.0104 mL	0.0522 mL	0.1044 mL	0.2611 mL

Keywords

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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YM458

MCE Bioactive Compound Library

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

YM458 Related Classifications

HY-146999 Related Classifications