货号: | R10048 |
CAS号: | 610798-31-7 |
规格: | 98% |
生物活性
Icotinib是一种有效的,特异性EGFR抑制剂,IC50为5 nM,包括EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M)和EGFR(T790M, L858R)。Icotinib抑制EGFR活性,IC50为5 nM,这种作用具有剂量依赖性,62.5 nM时则完全抑制。Icotinib选择性地仅抑制EGFR成员,包括野生型和突变体,抑制功效为61-99%。Icotinib作用于人类表皮样癌A431细胞,抑制EGFR调节的细胞内酪氨酸磷酸化,这种作用具有剂量依赖性。
实验操作 来自于公开的文献,仅供参考
细胞实验 | |
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细胞系 | A431 cell line |
方法 | MTT assay Cells (103/well) were seeded into 96-well plates in RPMI-1640 medium containing 10% FBS and grown in a 5% CO2 incubator at 37 ◦C. After 24 h, cells were treated with Icotinib at 0, 0.78, 1.56, 3.125, 6.25, 12.5 or 25 µM for 96 h. Cell proliferation was calculated by subtracting the mean absorbance value on day 0 from the mean absorbance value on day 4. |
浓度 | 0, 0.78, 1.56, 3.125, 6.25, 12.5 or 25 µM |
处理时间 | 96h |
动物实验 | |
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动物模型 | mice bearing A431, A549, H460 and HCT8 tumor xenografts |
配制 | 0.5% CMCNa |
剂量 | 30 mg/kg once a week |
给药处理 | i.p. |
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,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。
化学数据
分子量 | 391.4 |
分子式 | C22H21N3O4 |
CAS号 | 610798-31-7 |
纯度 | >98% |
溶解性(25°C) | DMSO |
储存和运输条件 | -20°C 冷藏长期储存 常温运输及临时存放 |
化学名称 |
参考文献
Effect of the CYP2C19 genotype on the pharmacokinetics of icotinib in healthy male volunteers.
Ruan CJ, et al. Eur J Clin Pharmacol. 2012 May 15. PMID: 22585284.
Effects of icotinib, a novel epidermal growth factor receptor tyrosine kinase inhibitor, in EGFR-mutated non-small cell lung cancer.
Yang G, et al. Oncol Rep. 2012 Jun;27(6):2066-72. PMID: 22446631.
Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies.
Tan F, et al. Lung Cancer. 2012 May;76(2):177-82. PMID: 22112293.
Phase I trial of icotinib, a novel epidermal growth factor receptor tyrosine kinase inhibitor, in Chinese patients with non-small cell lung cancer.
Wang HP, et al. Chin Med J (Engl). 2011 Jul 5;124(13):1933. PMID: 22088449.
Phase I study of icotinib hydrochloride (BPI-2009H), an oral EGFR tyrosine kinase inhibitor, in patients with advanced NSCLC and other solid tumors.
Zhao Q, et al. Lung Cancer. 2011 Aug;73(2):195-202. PMID: 21144613.