RUNX1/ETO-IN-1
Based on 1 Customer Validation
RUNX1/ETO-IN-1 is a RUNX1-ETO oncogenic fusion protein inhibitor that specifically targets the NHR2 oligomerization domain. RUNX1/ETO-IN-1 directly interacts with the NHR2 (KD,app = 39 μM). RUNX1/ETO-IN-1 exhibits anti-leukemic activity by inducing apoptosis and promoting differentiation in RUNX1/ETO-translocated AML cells. RUNX1/ETO-IN-1 remains essentially uncharged at physiological pH, demonstrating superior membrane permeability.
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- 純度 : 91.18%
- CAS 番号: 923865-06-9
- 分子式: C21H25N3O3S
- 分子量:399.51
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
生物活性
製品説明
体外実験
RUNX1/ETO-IN-1 (Cmpound M23) (96 h) Inhibits cell viability with an IC50 of 62.14 µM in the AML cell line SKNO-1 carrying the t(8;21) translocation that results in RUNX1/ETO[1].
RUNX1/ETO-IN-1 (20-200 µM) reduces the thermal stability of NHR2 (ΔTm = -1.6°C) in a concentration-dependent manner, likely by interfering with the tetramer-dimer equilibrium[1].
RUNX1/ETO-IN-1 (50-100 µM, 24 h) arrests cell cycle and potential induction of apoptosis in SKNO-1 cells, but not in THP-1 cells[1].
RUNX1/ETO-IN-1 (50-100 µM, 24 h) induces apoptosis in SKNO-1 cells by increasing caspase-3 and -7 activity but not in THP-1 and healthy NC-NC control cells[1].
RUNX1/ETO-IN-1 (25-50 µM, 3 days) promotes differentiation in SKNO-1 cells by increasing CD11b expression, but not in K562 and THP-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RUNX1/ETO-negative THP-1, K562, HL-60 cells, RUNX1/ETO-dependent SKNO-1 cells, B-lymphoblastoid cells
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Concentration:1-100 μM
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Incubation Time:72 h
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Result:Showed the highest sensitivity to SKNO-1 cells
Affected RUNX1/ETO-negative THP-1, K562, and HL-60 cells slightly
Did not affect B-lymphoblastoid cells
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Cell Line:RUNX1/ETO-negative THP-1 and RUNX1/ETO-positive SKNO-1 cells
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Concentration:50, 100 μM
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Incubation Time:24 h
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Result:Induced an accumulation in the subG1 and G1 phases, along with a reduction in the S and G2/M phases in the RUNX1/ETO-positive SKNO-1 cells and did not affect the cell cycle phase in the RUNX1/ETO-negative THP-1 cells.
化学情報
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CAS 番号 923865-06-9
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性状 Solid
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分子量 399.51
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分子式 C21H25N3O3S
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Color Light yellow to brown
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SMILES
CC1=CSC2=NC(CNC(C(C)C)C3=CC4=C(OCCCO4)C=C3)=CC(N12)=O
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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 In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 25 mg/mL (62.58 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 (275 KB)
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SDS (251 KB)
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- 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 | 2.5031 mL | 12.5153 mL | 25.0307 mL | 62.5767 mL |
| 5 mM | 0.5006 mL | 2.5031 mL | 5.0061 mL | 12.5153 mL | |
| 10 mM | 0.2503 mL | 1.2515 mL | 2.5031 mL | 6.2577 mL | |
| 15 mM | 0.1669 mL | 0.8344 mL | 1.6687 mL | 4.1718 mL | |
| 20 mM | 0.1252 mL | 0.6258 mL | 1.2515 mL | 3.1288 mL | |
| 25 mM | 0.1001 mL | 0.5006 mL | 1.0012 mL | 2.5031 mL | |
| 30 mM | 0.0834 mL | 0.4172 mL | 0.8344 mL | 2.0859 mL | |
| 40 mM | 0.0626 mL | 0.3129 mL | 0.6258 mL | 1.5644 mL | |
| 50 mM | 0.0501 mL | 0.2503 mL | 0.5006 mL | 1.2515 mL | |
| 60 mM | 0.0417 mL | 0.2086 mL | 0.4172 mL | 1.0429 mL |
RUNX1/ETO-IN-1 関連分類
HY-174367 関連分類
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