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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.16%
- CAS 番号: 2770108-93-3
- 分子式: C53H61ClN8O5S
- 分子量:957.62
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Histone Methyltransferase アイソフォーム固有の製品をすべて表示
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生物活性
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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.
化学情報
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CAS 番号 2770108-93-3
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性状 Solid
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分子量 957.62
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
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 関連分類
HY-146999 関連分類
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