Pelitinib (EKB-569)
(Synonyms: 培利替尼; EKB-569; WAY-EKB 569) 目录号 : GC17473
An EGFR receptor tyrosine kinase inhibitor
Cas No.:257933-82-7
Sample solution is provided at 25 µL, 10mM.
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Pelitinib (also known as EKB-569), a 3-cyanoquinoline, is a potent, and irreversible inhibitor of epidermal growth factor receptor (EGF-R) tyrosine kinase that inhibits the activity of EGF-R with the half maximal inhibition concentration IC50 value of 38.5 nM in vitro [1].
Pelitinib has been found to exert a potent anti-proliferative activity against tumor cells overexpressing EGF-R, including NHEK, A431 and MDA-468 cells, with IC50 values of 61 nM, 125 nM and 260 nM respectively; while it has also been found to potently inhibit EGF-induced phosphorylated EGF-R (pEGF-R) in A431 and NHEK cells with IC50 values ranging from 20 nM to 80 nM [2].
References:
[1] Torrance CJ, Jackson PE, Montgomery E, Kinzler KW, Vogelstein B, Wissner A, Nunes M, Frost P, Discafani CM. Combinatorial chemoprevention of intestinal neoplasia. Nat Med. 2000 Sep;6(9):1024-8.
[2] Nunes M, Shi C, Greenberger LM. Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human keratinocytes. Mol Cancer Ther. 2004 Jan;3(1):21-7.
Cell experiment: | For experiments using cells in culture, A431 cells or 3T3/c-erbB-2 cells over-expressing c-erbB2 are are treated with various concentrations of EKB-569 for 2.75 h before co-incubation with 100 ng/mL EGF (A431 cells) or no growth factor (3T3/c-erbB-2 cells) for 0.25 h. Cells are ished twice with cold phosphate-buffered saline (PBS) before adding to lysis buffer for 20 min on ice, before immunoprecipitation and SDS–PAGE-immunoblotting[1]. |
Animal experiment: | Mice: For in vivo experiments, athymic nu/nu female mice are implanted subcutaneously with 5×106 A431 tumor cells. When tumors reach a mass of 200-300 mg, animals are treated with a single dose of 10 mg/kg EKB-569 in pH 2.0 water per gavage. Tumors from control and drug-treated animals are excised and minced into 1-mm pieces for anlysis[1]. |
References: [1]. Torrance CJ, et al. Combinatorial chemoprevention of intestinal neoplasia. Nat Med. 2000 Sep;6(9):1024-8. | |
| Cas No. | 257933-82-7 | SDF | |
| 别名 | 培利替尼; EKB-569; WAY-EKB 569 | ||
| 化学名 | (E)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide | ||
| Canonical SMILES | CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)F)Cl)C#N)NC(=O)C=CCN(C)C | ||
| 分子式 | C24H23ClFN5O2 | 分子量 | 467.92 |
| 溶解度 | ≥ 11.7mg/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 | 2.1371 mL | 10.6856 mL | 21.3712 mL |
| 5 mM | 0.4274 mL | 2.1371 mL | 4.2742 mL |
| 10 mM | 0.2137 mL | 1.0686 mL | 2.1371 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet