NRC-2694
目录号 : GC33131NRC-2694是一种表皮生长因子受体(EGFR)拮抗剂,具有抗癌、抗增殖的活性。
Cas No.:936446-61-6
Sample solution is provided at 25 µL, 10mM.
NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties.
NRC-2694 at 80 ng (190 nm) concentrations causes comparable inhibition of EGFR expression[1].
In toxicity studies, the maximum tolerated dose of NRC-2694 in male and female mice is 2000 mg/kg (po). NRC-2694 (10 mg/kg) regresses the tumor in mice[1].
[1]. Ramanadham Jyothi Prasad, et al. 6-7,dialkoxy quinazoline derivatives useful for treatment of cancer related disorders. US 8143250 B2
Cell experiment: | The in vitro invasiveness of H1299 and A549 cells in the presence of various concentrations of NRC compounds (as determined by MTT assay) is assessed using a modified Boyden chamber assay. Cells are treated with these compounds for 48 hr. 1×106 cells are suspended in 600 μL of serum-free medium supplemented with 0.2% BSA and placed in the upper compartment of the transwell chambers coated with matrigel (0.7 mg/mL). The lower compartment of the chamber is filled with 200 μL of serum medium and the cells are allowed to migrate for 24 h. after incubation, the cells are fixed and stained with Hema-3 and quantified. The migrated cells are quantified as percent invasion. |
Animal experiment: | Mice: Nude mice are implanted with 2×106 A549 cells in the right hind limb flank. Upon the observance of a tumour (>2 mm), mice are given oral or ip treatments of the test compounds including erlotinib HCl used as positive control. A dose of 100 mg/kg of erlotinib HCl is identified as the base line dose. |
References: [1]. Ramanadham Jyothi Prasad, et al. 6-7,dialkoxy quinazoline derivatives useful for treatment of cancer related disorders. US 8143250 B2 |
Cas No. | 936446-61-6 | SDF | |
Canonical SMILES | COC1=CC2=NC=NC(NC3=CC=CC(C#C)=C3)=C2C=C1OCCCN4CCOCC4 | ||
分子式 | C24H26N4O3 | 分子量 | 418.49 |
溶解度 | DMSO: 250 mg/mL (597.39 mM) | 储存条件 | Store at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.3895 mL | 11.9477 mL | 23.8954 mL |
5 mM | 0.4779 mL | 2.3895 mL | 4.7791 mL |
10 mM | 0.239 mL | 1.1948 mL | 2.3895 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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