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同义名 : | - |
CAS号 : | 292053-42-0 | |
货号 : | A1234954 | |
分子式 : | C15H12N2O5S | |
纯度 : | 99% | |
分子量 : | 332.33 | |
MDL号 : | MFCD01847328 | |
存储条件: |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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溶解度 : | - | |
动物实验配方: |
生物活性 | |||
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描述 | Rearrangement of the mixed lineage leukemia (MLL, KMT2A) gene occurs in 5–10% of acute leukemias and is especially prevalent in infant acute leukemias (up to 70% of cases). The MLL-rearranged (MLL-r) leukemia subtype is characterized by its aggressive nature, resistance to therapy and typical occurrence of early relapse. CCI-006 is a novel inhibitor of MLL-r and CALM-AF10 translocated leukemias that share common leukemogenic pathways. CCI-006 (10 μM; 72 h) demonstrated a selective cytotoxic effect against 3 out of 4 tested MLL-r leukemia cell lines, without significantly affecting the viability of MLL-wt leukemia (n = 6) and solid tumor (n = 4) cell lines, or noncancerous cells (n = 3). CCI-006 reduced the viability of 7 out of 11 (64%) “sensitive” MLL-r leukemia cell lines to below 85% of that of vehicle-treated cells at a 10 µM dose, including cell lines derived from infant (younger than 1 year) or pediatric leukemia patients with chemo-resistant disease. CCI-006 significantly increased the percentage of cells expressing cell surface Annexin V (marker of apoptosis) in sensitive MLL-r leukemia cells within a few hours of treatment. In addition, in a JC-1 assay for mitochondrial membrane depolarization, CCI-006 induced mitochondrial depolarization in a dose-dependent manner within 1 h of treatment[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.01mL 0.60mL 0.30mL |
15.05mL 3.01mL 1.50mL |
30.09mL 6.02mL 3.01mL |
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