RG-14620
(Synonyms: Tyrphostin RG14620) 目录号 : GC10217
An inhibitor of EGF receptor kinase
Cas No.:136831-49-7
Sample solution is provided at 25 µL, 10mM.
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RG-14620 is a tyrosine kinase and epidermal growth factor (EGF) receptor [1].
Protein tyrosine kinases (PTKs) have been involved in regulating cell proliferation, cell differentiation, and signaling processes in the immune system. Dysfunction of protein tyrosine kinases result in inflammatory responses and diseases including cancer, atherosclerosis, and psoriasis [2]. The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein. Activation of EGFR results in autophosphorylation of receptor tyrosine kinase and has been involved in regulating cellular proliferation, differentiation, and survival. Overexpression of EGFR has been identified in a variety of tumor cell lines and has been associated with poor prognosis and decreased survival [3].
RG-14620 inhibited the activity of epidermal growth factor (EGF) receptor kinase with an IC50 value of 3 μM in HT-22 cells [1]. RG-14620 suppressed not only EGF-stimulated cancer cell proliferation in vitro but also tumor growth in nude mice [4]. Tyrphostin RG-14620 dose-dependently inhibited the EGFR-associated tyrosine kinase with half maximal inhibition at 7 μM [5].
References:
[1] Sagara, Y. , Ishige, K., Tsai, C., et al. Tyrphostins protect neuronal cells from oxidative stress. The Journal of Biological Chemisty, 277(39), 36204-36215(2002).
[2] Levitzki A, Gazit A. Tyrosine kinase inhibition: an approach to drug development[J]. Science, 1995, 267(5205): 1782.
[3] Herbst R S. Review of epidermal growth factor receptor biology[J]. International Journal of Radiation Oncology Biology Physics, 2004, 59(2): S21-S26.
[4] Yoneda T, Lyall R M, Alsina M M, et al. The antiproliferative effects of tyrosine kinase inhibitors tyrphostins on a human squamous cell carcinoma in vitro and in nude mice[J]. Cancer research, 1991, 51(16): 4430-4435.
[5] Piontek M, Hengels K J, Porschen R, et al. Antiproliferative effect of tyrosine kinase inhibitors in epidermal growth factor-stimulated growth of human gastric cancer cells[J]. Anticancer research, 1992, 13(6A): 2119-2123.
Cell experiment: | MH-85 cells and HER 14 cells are plated in complete medium, either αMEM or DMEM, respectively, supplemented with 10% FCS. After overnight culture, the culture medium is switched to αMEM supplemented with 0.2% PCS and 50 ng/mL EGF (MH-85) or DMEM supplemented with 0.5% PCS and 50 ng/mL EGF (HER14). The cells are cultured in this medium in the presence or absence of increasing concentrations of RG-13022 or RG-14620 for 10 days. At the end of culture, the cells are fixed with 4% (v/v) formaldehyde in calcium-magnesium-free phosphate-buffered saline for 15 min at room temperature and stained with hematoxylin. Numbers of colonies including more than 20 cells in each well are counted under the microscope[2]. |
Animal experiment: | Mice: RG14620 in 0.1 mL 100% DMSO is injected i.p. twice a day from 1day after MH-85 tumor inoculation. Control animals are given the same vehicle[1]. |
References: [1]. Sagara Y, et al. Tyrphostins protect neuronal cells from oxidative stress. J Biol Chem. 2002 Sep 27;277(39):36204-15. | |
| Cas No. | 136831-49-7 | SDF | |
| 别名 | Tyrphostin RG14620 | ||
| 化学名 | α-[(3,5-dichlorophenyl)methylene]-3-pyridineacetonitrile | ||
| Canonical SMILES | ClC1=CC(/C=C(C#N)/C2=CN=CC=C2)=CC(Cl)=C1 | ||
| 分子式 | C14H8Cl2N2 | 分子量 | 275.1 |
| 溶解度 | ≤1mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide | 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 | 3.635 mL | 18.1752 mL | 36.3504 mL |
| 5 mM | 0.727 mL | 3.635 mL | 7.2701 mL |
| 10 mM | 0.3635 mL | 1.8175 mL | 3.635 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