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RG13022

Catalog No. T3545   CAS 136831-48-6
Synonyms: RG 13022, Tyrphostin RG13022

RG13022 (Tyrphostin RG13022) is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor (IC50: 4 μM).

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RG13022 Chemical Structure
RG13022, CAS 136831-48-6
Pack Size Availability Price/USD Quantity
2 mg In stock $ 39.00
5 mg In stock $ 55.00
10 mg In stock $ 80.00
25 mg In stock $ 189.00
50 mg In stock $ 320.00
100 mg In stock $ 506.00
1 mL * 10 mM (in DMSO) In stock $ 58.00
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Purity: 98.38%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description RG13022 (Tyrphostin RG13022) is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor (IC50: 4 μM).
Targets&IC50 EGF:4 μM
In vitro RG13022 suppresses EGF-stimulated cancer cell proliferation. In a cell-free reaction, RG13022 inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates (IC50: 4 μM). RG13022 inhibits colony formation (IC50: 1 μM) and DNA synthesis (IC50: 3 μM) by HER 14 cells (stimulated by 50 ng/mL EGF), in a dose-dependent manner. RG-13022 inhibits not only EGF-induced growth but also growth stimulated by insulin, insulin-like growth factor I, insulin-like growth factor II, or transforming growth factor alpha. RG-13022 also totally blocks estrogen-stimulated phosphorylation of the EGF receptor, as well as estrogen-induced cell proliferation, suggesting that functioning TK pathways are required for estrogen action.
In vivo RG13022 suppresses tumor growth in nude mice. It also increases the lifespan of these tumor-bearing nude mice.
Cell Research 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].
Synonyms RG 13022, Tyrphostin RG13022
Molecular Weight 266.29
Formula C16H14N2O2
CAS No. 136831-48-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (187.76 mM)

TargetMolReferences and Literature

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. 2. Reddy KB, et al. Inhibition of breast cancer cell growth in vitro by a tyrosine kinase inhibitor. Cancer Res. 1992 Jul 1;52(13):3636-41. 3. Nguyen D J M, Theodoropoulos G, Li Y Y, et al. Targeting the kynurenine pathway for the treatment of cisplatin-resistant lung cancer[J]. Molecular Cancer Research. 2020, 18(1): 105-117.

TargetMolCitations

1. Nguyen D J M, Theodoropoulos G, Li Y Y, et al. Targeting the kynurenine pathway for the treatment of cisplatin resistant lung cancer. Molecular Cancer Research. 2019: molcanres. 0239.2019

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Inhibitor Library Anti-Liver Cancer Compound Library Anti-Colorectal Cancer Compound Library Anti-Breast Cancer Compound Library Covalent Inhibitor Library Angiogenesis related Compound Library Bioactive Compound Library

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Keywords

RG13022 136831-48-6 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR HER1 Inhibitor RG 13022 Tyrphostin RG-13022 inhibit ErbB-1 Tyrphostin RG13022 Tyrphostin RG 13022 RG-13022 Epidermal growth factor receptor inhibitor

 

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