RG 13022 (Synonyms: Tyrphostin RG13022) |
Catalog No.GC12038
One-Click Copy Product Info
|
EGFR tyrosine kinase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 136831-48-6
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
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.
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. | |
| Cas No. | 136831-48-6 | SDF | |
| Synonyms | Tyrphostin RG13022 | ||
| Chemical Name | (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 | ||
| Formula | C16H14N2O2 | M.Wt | 266.29 |
| Solubility | ≥ 26.6mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.7553 mL | 18.7765 mL | 37.553 mL |
| 5 mM | 751.1 μL | 3.7553 mL | 7.5106 mL |
| 10 mM | 375.5 μL | 1.8777 mL | 3.7553 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)