1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. RG13022

RG13022 (Synonyms: Tyrphostin RG13022; )

Cat. No.: HY-101429 Purity: >95.0%
Handling Instructions

RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.

For research use only. We do not sell to patients.

RG13022 Chemical Structure

RG13022 Chemical Structure

CAS No. : 136831-48-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
2 mg USD 50 In-stock
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5 mg USD 70 In-stock
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10 mg USD 100 In-stock
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25 mg USD 230 In-stock
Estimated Time of Arrival: December 31
50 mg USD 390 In-stock
Estimated Time of Arrival: December 31
100 mg USD 620 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.

IC50 & Target

IC50: 4 μM (EGF receptor autophosphorylation)[1]

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 with an IC50 of 4 μM. RG13022 inhibits colony formation and DNA synthesis by HER 14 cells, which were stimulated by 50 ng/mL EGF, in a dose-dependent manner. The IC50s are 1 and 3 μM for HER 14 colony formation and DNA synthesis, respectively[1]. 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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

RG13022 suppresses tumor growth in nude mice. RG13022 also increases the life span of these tumor-bearing nude mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

266.29

Formula

C₁₆H₁₄N₂O₂

CAS No.

136831-48-6

SMILES

N#C/C(C1=CC=CN=C1)=C/C2=CC=C(OC)C(OC)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

RG13022Tyrphostin RG13022RG 13022RG-13022Tyrphostin RG 13022Tyrphostin RG-13022EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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RG13022
Cat. No.:
HY-101429
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