Name | tyrphostin rg 14620 |
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Synonyms |
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 |
Description | RG14620 is an EGFR inhibitor with an IC50 of 3 μM. |
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Related Catalog | |
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 |
Density | 1.4±0.1 g/cm3 |
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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 |
Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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Safety Phrases | S22-S24/25 |
RIDADR | NONH for all modes of transport |