YM458
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.16%
- CAS No.: 2770108-93-3
- Formula: C53H61ClN8O5S
- Molecular Weight:957.62
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
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Biological Activity
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EZH2 |
EZH2 490 nM (IC50) |
BRD4 34 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| ASPC1 | IC50 |
0.69 μM
Compound: 27
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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
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[PMID: 37156182] |
| ASPC1 | IC50 |
0.69 μM
Compound: D7; YM458
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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
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[PMID: 35500243] |
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.
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Cell Line:AsPC-1[1]
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Concentration:1 μM
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Incubation Time:72 hours
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Result:Decreased the degree of H3K27me3 and c-Myc significantly.
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Cell Line:AsPC-1, SW1990, CFPAC-1, A549, HCC827, H1650, H292, H460, DLD1, HCT116, and RKO[1]
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Concentration:0-30 μM
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Incubation Time:4 or 6 days
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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.
Pharmacokinetic Parameters of YM458 in Female BALB/c mice[1].
| IP (80 mg/kg) | PO (80 mg/kg) | |
| t1/2 (h) | 3.81 | 4.16 |
| Tmax (h) | 1 | 1 |
| Cmax (ng/mL) | 27126.3 | 4383.6 |
| AUC0-24 (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.
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Animal Model:BALB/c nude mice (injected with A549 or AsPC-1)[1]
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Dosage:60 mg/kg
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Administration:IP; every other day, for 38 days
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Result:Prevented tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells.
Chemical Information
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CAS No. 2770108-93-3
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Appearance Solid
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Molecular Weight 957.62
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Formula C53H61ClN8O5S
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Color White to off-white
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (280 KB)
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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)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| 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 |
YM458 Related Classifications
HY-146999 Related Classifications
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