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  • DC Chemicals Limited
  • China
  • Product Name: RG-13022
  • Price: $300.0/100mg $600.0/250mg $1200.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

136831-48-6

136831-48-6 structure
136831-48-6 structure
  • Name: RG-13022
  • Chemical Name: tyrphostin rg 13022
  • CAS Number: 136831-48-6
  • Molecular Formula: C16H14N2O2
  • Molecular Weight: 266.29500
  • Catalog: Research Areas Cancer
  • Create Date: 2018-10-21 20:03:07
  • Modify Date: 2024-01-02 11:46:45
  • RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.

Name tyrphostin rg 13022
Synonyms 2-(3,4'-Dimethoxyphenyl)-1-(3''-pyridinyl)acrylonitrile
MFCD00236444
RG-13022
Description RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
Related Catalog
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].
In Vivo RG13022 suppresses tumor growth in nude mice. RG13022 also increases the life span of these tumor-bearing nude mice[1].
Cell Assay 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 Admin 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.

[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.

Density 1.172g/cm3
Boiling Point 423.8ºC at 760mmHg
Melting Point 118 °C
Molecular Formula C16H14N2O2
Molecular Weight 266.29500
Flash Point 210.1ºC
Exact Mass 266.10600
PSA 55.14000
LogP 3.16298
Vapour Pressure 2.18E-07mmHg at 25°C
Index of Refraction 1.605
Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Safety Phrases S22-S24/25
RIDADR NONH for all modes of transport
Precursor  2

DownStream  0