RG 13022
(Synonyms: Tyrphostin RG13022) 目录号 : GC12038
An inhibitor of EGF receptor kinase
Cas No.:136831-48-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | 40 mM stock solutions of RG13022 is made in 100% DMSO and diluted with the culture medium before addition to the cells. MH-85 cells and HER 14 cells are plated in culture 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 and stained with hematoxylin. Numbers of colonies including more than 20 cells in each well are counted under the microscope[1]. |
Animal experiment: | Mice: MH-85 tumors 5 mm in diameter are inoculated s.c. into the right dorsal portion of 4- to 6-week-old male BALB/c nu/nu mice. RG-13022 or RG-14620 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. Tumor sizes are measured once a week under anesthesia with nembutal (0.05 mg/g body weight, i.p.) and calculated[1]. |
References: [1]. Yoneda T, et al. The antiproliferative effects of tyrosine kinase inhibitors tyrphostins on a human squamous cell carcinoma in vitro and in nude mice. Cancer Res. 1991 Aug 15;51(16):4430-5. | |
IC50: 5 μM for EGFR
RG13022 is a EGFR tyrosine kinase inhibitor.
Increased expression of various growth factor receptors including EGFR has been observed in human tumours. One therapeutic strategy for overcoming EGF autocrine control of tumour growth is to inhibit EGFR protein tyrosine kinase.
In vitro: RG13022 had a dose-dependent, antiproliferative effect on gastric cell lines when grown either in serum-free conditions or in the presence of FCS. Western blotting showed that RG13022 treatment led to an inhibition of the EGFr phosphorylation in A431 cells and both EGFr and c-erbB-2 in MKN45 cells. Furthermore, investigation of intracellular signalling pathways suggested that alterations in intracellular signalling were responsible for the actions of RG 13022 in these cells [1].
In vivo: In rats, RG13022 showed rapid bi-exponential elimination from plasma with a terminal half-life of 50.4 min. RG13022 plasma concentrations were less than 1 μM by 20 min after injection. In addition, RG13022 had no influence on the growth of HN5 tumours when administered chronically, starting either on the tumour inoculation day or after establishment of tumour xenografts. The rapid in-vivo elimination of RG13022 had potential significance to its development, as plasma concentrations fell below that required for in-vitro activity by 20 min after injection [2].
Clinical trial: Up to now, RG13022 is still in the preclinical development stage.
References:
[1] McLaughlin M,Brunton V,Morrison V,Rae A,Cooke T,Bartlett J. Growth inhibition of gastric cancer cell lines by the tyrphostin RG13022 and its effects on intracellular signalling. Int J Oncol.1996 Mar;8(3):589-96.
[2] McLeod HL,Brunton VG,Eckardt N,Lear MJ,Robins DJ,Workman P,Graham MA. In vivo pharmacology and anti-tumour evaluation of the tyrphostin tyrosine kinase inhibitor RG13022. Br J Cancer.1996 Dec;74(11):1714-8.
| Cas No. | 136831-48-6 | SDF | |
| 别名 | Tyrphostin RG13022 | ||
| 化学名 | (E)-3-(3,4-dimethoxyphenyl)-2-(pyridin-3-yl)acrylonitrile | ||
| Canonical SMILES | N#C/C(C1=CC=CN=C1)=C/C2=CC=C(C(OC)=C2)OC | ||
| 分子式 | C16H14N2O2 | 分子量 | 266.29 |
| 溶解度 | ≥ 26.6mg/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 | 3.7553 mL | 18.7765 mL | 37.553 mL |
| 5 mM | 0.7511 mL | 3.7553 mL | 7.5106 mL |
| 10 mM | 0.3755 mL | 1.8777 mL | 3.7553 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。
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