CCI-006

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Chemical Structure| 292053-42-0 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
溶解度 :

DMSO: 85 mg/mL(255.77 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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].
实验方案
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
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