生物活性
PQ 401抑制IGF-1R区域自磷酸化,IC50为低于1 μM。PQ 401是IGF-1R 抑制剂,浓度<100 nM时,抑制IGF-IR激酶域的自磷酸化,IC50 < 1μM. PQ 401显著降低MCF-7细胞增殖,IC50为8 μM。PQ 401也抑制MCNeuA细胞生长,IC50为15 μM。PQ 401作用于MCF-7 细胞,抑制IGF-I调节的抗凋亡途径。
化学数据
分子量 | 341.79 |
分子式 | C18H16ClN3O2 |
CAS号 | 196868-63-0 |
纯度 | 99.89% |
溶解性(25°C) | DMSO 15 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 |
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细胞系 | MCF-7 cells |
方法 | Effects of Diaryl Urea on IGF-I Stimulated Proliferation of Breast Cancer Cells
MCF-7 cells were harvested by washing thrice with PBS and dissociating with 1 mL 0.05% trypsin. Cells were resuspended in 5 mL defined medium (1:1 Ham's F12/DMEM 4.5 g/L glucose; 1 mg/mL bovine serum albumin; 10 μg/mL transferrin; 15 mmol/L HEPES pH 7.2; 2 mmol/L L-glutamine; 100 units/mL penicillin G; 100 μg/mL streptomycin SO4; 2.5 μg/mL fungizone) containing 200 μg soybean trypsin inhibitor. Cells were plated in 96-well collagen-coated plates (Sigma) at a density of 5,000 per well in 100-μL medium. Twenty hours later, defined medium with or without IGF-I (10 nmol/L) was added. Four hours later, PQ401 diluted in defined medium was added. Plates were harvested on day 3, as described above, for determination of cell number by CyQuant assay. |
浓度 | 0, 2.5, 5, 7.5, 15, 30μM |
处理时间 | 3 days |
动物实验 |
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动物模型 | MCNeuA tumor cells bearing mice model |
配制 | 8% polysorbate 80/ethanol/PBS |
剂量 | 50 or 100 mg/kg |
给药处理 | i.p. thrice a week |
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 |
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1 mM | 2.9258 mL | 14.6289 mL | 29.2577 mL |
5 mM | 0.5852 mL | 2.9258 mL | 5.8515 mL |
10 mM | 0.2926 mL | 1.4629 mL | 2.9258 mL |