Icotinib
(Synonyms: 埃克替尼; BPI-2009) 目录号 : GC17982
An EGFR inhibitor
Cas No.:610798-31-7
Sample solution is provided at 25 µL, 10mM.
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Icotinib is a potent and specific EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor (IC50 = 5 nM) [1]
EGFR are family of receptor tyrosine kinase that is a transmembrane protein involved in the regulation of cell proliferation, motility and apoptosis. EGFR are expressed in various human cancer types, including breast, head & neck, NSCLC (non-small cell lung cancer) and ovarian caners. [1]
In human epidermoid carcinoma A431 cell line, Icotinib inhibited EGF-induced EGFR phosphorylation in a dose-dependent manner. Icotinib inhibited tyrosine phosphorylation of a variety of intracellular proteins. [1]
In different types of tumor xenograft mice models, Icotinib inhibited tumor growth in a dose-dependent manner without pronounced adverse effect in body weight loss and toxicity signs. In a randomized, double-blind, Gefitinib as control and multi-center phase III trial, Icotinib demonstrated efficacy on NSCLC in advanced stage. [1]
Reference:
[1] Tan F, Shen X, Wang D, Xie G, Zhang X, Ding L, Hu Y, He W, Wang Y, Wang Y. Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies. Lung Cancer. 2012 May;76(2):177-82.
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Kinase experiment: |
In the in vitro kinase assays, 2.4 ng/μL EGFR protein is mixed with 32 ng/μL Crk in 25 μL kinase reaction buffer containing 1 μM cold ATP and 1 μCi32P-γ-ATP. The mix is incubated with Icotinib at 0, 0.5, 2.5, 12.5 or 62.5 nM on ice for 10 min followed by incubation at 30°C for 20 min. After quenching with SDS sample bufferat 100°C for 4 min, the protein mix is resolved by electrophoresis in a 10% SDS-PAGE gel. The dried gel is then exposed to detect radioactivity. Quantification is performed by software[1]. |
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Cell experiment: |
Cells (1000/well) are 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 are treated with Icotinib at 0, 0.78, 1.56, 3.125, 6.25, 12.5 or 25 μM for 96 h. Cell proliferation is calculated by subtracting the mean absorbance value on day 0 from the mean absorbance value on day 4[1]. |
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Animal experiment: |
Mice: The effect of three doses of Icotinib (30, 60, and 120 mg/kg/dose p.o. qd) on antitumor activity and survival is determined in mice bearing A431, A549, H460 and HCT8 tumor xenografts. Taxol (30 mg/kg/dose i.p. once a week) is employed in these experiments as a positive control group[1]. |
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References: [1]. Tan F, et al. Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies. Lung Cancer. 2012 May;76(2):177-82. |
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| Cas No. | 610798-31-7 | SDF | |
| 别名 | 埃克替尼; BPI-2009 | ||
| 化学名 | N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine | ||
| Canonical SMILES | [H]C1=C2OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC2=C([H])C3=NC([H])=NC(N([H])C4=C([H])C([H])=C([H])C(C#C[H])=C4[H])=C31 | ||
| 分子式 | C22H21N3O4 | 分子量 | 391.42 |
| 溶解度 | ≥ 129.6mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5548 mL | 12.774 mL | 25.548 mL |
| 5 mM | 0.511 mL | 2.5548 mL | 5.1096 mL |
| 10 mM | 0.2555 mL | 1.2774 mL | 2.5548 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet