| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
EGFR:3 μM (IC50, Cell Assay)
The primary target of RG 14620 is the Epidermal Growth Factor Receptor (EGFR), a receptor tyrosine kinase. It inhibits the kinase activity of EGFR, preventing its autophosphorylation and subsequent downstream signaling pathways such as JAK/STAT. |
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| ln Vitro |
In HER 14 cells stimulated by 50 ng/mL EGF, RG14620 suppresses DNA synthesis (IC50=1 μM) and colony formation (IC50=3 μM) in a dose-dependent manner. Additionally, in a dose-dependent manner, RG14620 inhibits DNA synthesis (IC50=1.25 μM) and colony formation (IC50=4 μM) in EGF-stimulated MH-85 cells. The irreversible growth-inhibitory effect of RG14620[2].
In cell-free assays, RG 14620 inhibits EGFR autophosphorylation with an IC50 of 4 µM. It also inhibits the activity of EGF receptor kinase in HT-22 cells with an IC50 of 3 µM. The compound demonstrates a dose-dependent inhibitory effect on its target enzyme. |
| ln Vivo |
At 200 g/mouse/day, RG14620 suppresses the formation of H-85 tumors in mice that are not clothed. Comparing mice to untreated MH-85 tumor-bearing animals, they consume more food, have less cachexia and hypercalcemia, and are more active[2].
In HER 14 cells stimulated by EGF, RG 14620 inhibits colony formation with an IC50 of 3 µM and DNA synthesis with an IC50 of 1 µM. It also suppresses colony formation and DNA synthesis in EGF-stimulated MH-85 cells. Furthermore, it inhibits the growth of human gastric cancer cells with an IC50 of 7 µM. |
| Enzyme Assay |
The standard cell-free assay involves incubating the EGFR kinase enzyme with a substrate (e.g., a peptide) and ATP in the presence of varying concentrations of RG 14620. The reaction is typically carried out in a buffer optimized for kinase activity. After incubation, the level of phosphorylated substrate is measured, often using an antibody-based detection method like ELISA or by quantifying radioactive phosphate incorporation.
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| 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 Protocol |
In in vivo models, RG 14620 is administered to nude mice bearing H-85 tumor xenografts at a dose of 200 µg/mouse/day. Tumor growth is monitored over time. Treated mice exhibit less cachexia and hypercalcemia, eat more food, and are more active than untreated tumor-bearing animals.
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| ADME/Pharmacokinetics |
The compound is soluble in DMSO at 33.33 mg/mL. For in vivo administration, it can be formulated in a vehicle such as 10% DMSO, 40% PEG300, 5% Tween-80, and 45% saline. This formulation yields a suspended solution at a concentration of 2.5 mg/mL.
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| Toxicity/Toxicokinetics |
Specific toxicity data for RG 14620 is limited. As an inhibitor of EGFR, which plays a role in normal cell function, potential toxicities may be related to on-target effects. In animal studies, the compound was tolerated at the doses used for efficacy, as treated mice showed improved overall health compared to controls.
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| References | |
| Additional Infomation |
3-(3,5-Dichlorophenyl)-2-(3-pyridyl)-2-acrylonitrile is a dichlorobenzene.
See also: RG 14620 (note moved to). RG 14620 is a research compound primarily used to study EGFR signaling and its role in cancer. Its ability to inhibit EGFR and modulate ABCG2 makes it a useful tool for studying drug resistance mechanisms. It has not been approved for clinical use and has not advanced to clinical trials for cancer therapy. |
| Molecular Formula |
C14H8CL2N2
|
|---|---|
| Molecular Weight |
275.13
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| Exact Mass |
274.006
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| Elemental Analysis |
C, 61.12; H, 2.93; Cl, 25.77; N, 10.18
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| CAS # |
136831-49-7
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| Related CAS # |
136831-49-7;
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| PubChem CID |
5353928
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
418.2±45.0 °C at 760 mmHg
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| Melting Point |
155 °C
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| Flash Point |
206.7±28.7 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.657
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| LogP |
4.47
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
18
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| Complexity |
348
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C([H])=C(C([H])=C(C=1[H])/C(/[H])=C(/C#N)\C1=C([H])N=C([H])C([H])=C1[H])Cl
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| InChi Key |
TYXIVBJQPBWBHO-QCDXTXTGSA-N
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| InChi Code |
InChI=1S/C14H8Cl2N2/c15-13-5-10(6-14(16)7-13)4-12(8-17)11-2-1-3-18-9-11/h1-7,9H/b12-4-
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| Chemical Name |
(E)-3-(3,5-dichlorophenyl)-2-pyridin-3-ylprop-2-enenitrile
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| Synonyms |
RG-14620 RG14620 RG 14620
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~121.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (9.09 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (9.09 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6346 mL | 18.1732 mL | 36.3465 mL | |
| 5 mM | 0.7269 mL | 3.6346 mL | 7.2693 mL | |
| 10 mM | 0.3635 mL | 1.8173 mL | 3.6346 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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