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CAS No.: 292053-42-0

CCI-006 Catalog No. CSN25545

CCI-006 is a novel inhibitor of MLL-rearranged and CALM-AF10 translocated leukemias, inhibiting mitochondrial respiration and inducing mitochondrial membrane depolarization and apoptosis in a subset (7/11, 64%) of MLL-rearranged leukemia cell lines within a few hours of treatment.

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400-920-2911

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技术信息

生物活性

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].
参考文献

[1] Somers K, Wen VW, Middlemiss SMC, et al. A novel small molecule that kills a subset of MLL-rearranged leukemia cells by inducing mitochondrial dysfunction. Oncogene. 2019;38(20):3824-3842

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0090 mL
- 15.0452 mL
- 30.0905 mL
- 5 mM
- 0.6018 mL
- 3.0090 mL
- 6.0181 mL
- 10 mM
- 0.3009 mL
- 1.5045 mL
- 3.0090 mL

技术信息

CAS号

292053-42-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H12N2O5S

运输

蓝冰

分子量

332.33

别名

溶解度

DMSO	83.33 mg/mL (250.7 mM)

动物实验配方

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