生物活性
CX-6258 inhibited Flt-3 and Pim-3 (IC50=0.134 and 0.016 uM). CX-6258 is a reversible inhibitor of Pim-1 (Ki=0.005 uM). CX-6258 shows robust antiproliferative potencies against all cell lines tested derived from human solid tumors and hematological malignancies. CX-6258 shows dose-dependent efficacy in mice bearing MV-4-11 xenografts, with 45% and 75% TGI at 50 and 100 mg/kg/day, respectively.
化学数据
| 分子量 | 461.94 |
| 分子式 | C26H24ClN3O3 |
| CAS号 | 1202916-90-2 |
| 纯度 | >99% |
| 溶解性（25°C） | DMSO ≥ 10 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | MV-4-11, SEM, EOL-1, MOLM-13, PL-21, THP-1, K562, MEG01, HL60 and U266 cells |
| 方法 | Cell Viability assay.
For proliferation assays, cells were plated at 5,000 to 20,000 cells per well in 96 well plates overnight before treatment for 96 hours with serially diluted compound or vehicle DMSO. Cell viability was measured after the addition of 10 μL Alamar Blue (Invitrogen) for 4 hours at 37?C. The GI50 was determined by calculating growth at each dose relative to vehicle treated cells and cell viability at the time of treatment. |
| 浓度 | 0~10 μM |
| 处理时间 | 96 h |
| 动物实验 |
|---|
| 动物模型 | MV-4-11 xenograft models in nude mice |
| 配制 | H2O |
| 剂量 | 50 or 100 mg/kg once daily over a period of 21 days |
| 给药处理 | PO |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1648 mL | 10.8239 mL | 21.6478 mL |
| 5 mM | 0.433 mL | 2.1648 mL | 4.3296 mL |
| 10 mM | 0.2165 mL | 1.0824 mL | 2.1648 mL |
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