RG14620

Names

[ Name ]:
RG14620

[Synonym ]:
MFCD00236445
3-Pyridineacetonitrile, α-[(3,5-dichlorophenyl)methylene]-, (αZ)-
2-(3',5'-Dichlorophenyl)-1-(3''-pyridinyl)acrylonitrile
(2Z)-3-(3,5-Dichlorophenyl)-2-(3-pyridinyl)acrylonitrile
3-Pyridineacetonitrile, α-[(3,5-dichlorophenyl)methylene]-, (αE)-
(2E)-3-(3,5-Dichlorophenyl)-2-(3-pyridinyl)acrylonitrile
3-Pyridineacetonitrile, α-((3,5-dichlorophenyl)methylene)-
RG-14620

Biological Activity

[Description]:

RG14620 is an EGFR inhibitor with an IC50 of 3 μM.

[Related Catalog]:

Research Areas >> Cancer

[Target]

EGFR:3 μM (IC50, Cell Assay)

[In Vitro]

RG14620 inhibits colony formation (IC50=3 μM) and DNA synthesis (IC50=1 μM) by HER 14 cells, which are stimulated by 50 ng/mL EGF, in a dose-dependent manner. RG14620 also suppresses colony formation(IC50=4 μM) and DNA synthesis (IC50=1.25 μM) by EGF-stimulated MH-85 cells in a dose-dependent manner. The growth-inhibitory effect of RG14620 irreversible[2].

[In Vivo]

RG14620, at a dose of 200 g/mouse/day inhibits H-85 tumor growth in nude mice. Mice show less cachexia and hypercalcemia, eat more food, and are more active than untreated MH-85 tumor-bearing animals[2].

[Cell Assay]

MH-85 cells and HER 14 cells are plated in complete medium, either αMEM or DMEM, respectively, supplemented with 10% FCS. After overnight culture, the culture medium is switched to αMEM supplemented with 0.2% PCS and 50 ng/mL EGF (MH-85) or DMEM supplemented with 0.5% PCS and 50 ng/mL EGF (HER14). The cells are cultured in this 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 in calcium-magnesium-free phosphate-buffered saline for 15 min at room temperature and stained with hematoxylin. Numbers of colonies including more than 20 cells in each well are counted under the microscope[2].

[Animal admin]

Mice: RG14620 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[1].

[References]

[1]. Sagara Y, et al. Tyrphostins protect neuronal cells from oxidative stress. J Biol Chem. 2002 Sep 27;277(39):36204-15.

[2]. 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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
418.2±45.0 °C at 760 mmHg

[ Melting Point ]:
155 °C

[ Molecular Formula ]:
C₁₄H₈Cl₂N₂

[ Molecular Weight ]:
275.133

[ Flash Point ]:
206.7±28.7 °C

[ Exact Mass ]:
274.006439

[ PSA ]:
36.68000

[ LogP ]:
4.47

[ Vapour Pressure ]:
0.0±1.0 mmHg at 25°C

[ Index of Refraction ]:
1.657

Safety Information

[ 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

Articles

Photoinstability of some tyrphostin drugs: chemical consequences of crystallinity.

Pharm. Res. 12(11) , 1708-15, (1995)

The purpose of this work was to study the photostability of the antiproliferative tyrphostin drug compounds RG 13022(I) and RG 14620(II) as a part of preformulation program.The compounds were exposed ...

Upregulation of retinoic acid receptor-beta by the epidermal growth factor-receptor inhibitor PD153035 is not mediated by blockade of ErbB pathways.

J. Cell Physiol. 211(3) , 803-15, (2007)

Inhibiting epidermal growth factor-receptor (ErbB-1) represents a powerful anticancer strategy. Activation of retinoid pathways is also in development for cancer treatment. Retinoic acid receptor-beta...

[Effect of signal transduction inhibitors on human endometrial carcinoma cells with differential PTEN gene expression].

Zhonghua Fu Chan Ke Za Zhi 44(9) , 681-5, (2009)

To investigate the apoptotic and proliferation effects of signal transduction inhibitors on human endometrial carcinoma cells with different PTEN gene expression.PTEN antisense oligonucleotide and pcD...