Home Protein Tyrosine Kinase EGFR inhibitor RG 13022

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RG 13022 EGFR inhibitor

Cat.No.S2115

RG 13022 (Tyrphostin RG13022) inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates with IC50 of 4 µM.
RG 13022 EGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 266.29

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Quality Control

Batch: S211501 DMSO]53 mg/mL]false]Ethanol]5 mg/mL]false]Water]Insoluble]false Purity: 99.28%
99.28

Chemical Information, Storage & Stability

Molecular Weight 266.29 Formula

C16H14N2O2

 

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 136831-48-6 -- Storage of Stock Solutions

Synonyms Tyrphostin RG13022 Smiles COC1=C(C=C(C=C1)C=C(C#N)C2=CN=CC=C2)OC

Solubility

In vitro
Batch:

DMSO : 53 mg/mL (199.03 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

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In vivo
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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 ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
EGFR
(Cell-free assay)
4 μM
In vitro

RG-13022 inhibits autophosphorylation of the EGF-receptor in HER 14 cells after an overnight incubation. The IC50 of RG-13022 is 5 µM. RG-13022 inhibits colony formation and DNA synthesis by HER 14 cells, which are stimulated by 50 ng/mL EGF, in a dose-dependent manner. The IC50 for RG-13022 is 1 µM for HER 14 colony formation and 3 µM for HER 14 DNA synthesis. RG-13022 also suppresses colony formation and DNA synthesis by EGF-stimulated MH-85 cells in a dose-dependent manner. The IC50 for RG-13022 on MH-85 cells is 7 µM for colony formation and 1.5 µM for DNA synthesis..
In vivo

RG-13022 (400 µg/mouse/day) significantly inhibits MH-85 tumour growth. Because of slower tumour growth, MH-85 tumour-bearing animals receiving injections of RG-13022 show less cachexia and hypercalcaemia, eat more food, and are more active than untreated MH-85 tumour-bearing animals. As a result of suppression of tumour growth, RG-13022 prolongs the life span of MH-85 tumour-bearing animals. Administration of mAb108 i.p. (1 mg/mouse/day) at 1, 5, and 10 days after MH-85 inoculation of RG-13022 (400 µg/mouse/day) for 14 days profoundly inhibits MH-85 growth in nude mice..
References

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