| 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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| 250mg |
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| 500mg |
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| Other Sizes |
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| Targets |
EGF receptor autophosphorylation (IC50 = 4 μM)
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|---|---|
| ln Vitro |
G-13022 prevents the EGF-receptor in HER 14 cells from becoming autophosphorylated after an overnight incubation. RG-13022 has an IC50 of 5 μM. When HER 14 cells are stimulated by 50 ng/mL EGF, RG-13022 inhibits colony formation and DNA synthesis in a dose-dependent manner. For HER 14 colony formation, RG-13022's IC50 is 1 μM, while for HER 14 DNA synthesis, it is 3 μM. Additionally, EGF-stimulated MH-85 cells' colony formation and DNA synthesis are suppressed by RG-13022 in a dose-dependent manner. For MH-85 cells, the IC50 values of RG-13022 are 7 μM for colony formation and 1.5 μM for DNA synthesis.[1]
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| ln Vivo |
RG-13022, at 400 μg/mouse/day, considerably suppresses the growth of MH-85 tumors. In comparison to untreated MH-85 tumor-bearing animals, animals receiving injections of RG-13022 exhibit less cachexia and hypercalcemia, eat more food, and exhibit greater levels of activity due to slower tumor growth. RG-13022 extends the life span of MH-85 tumor-bearing animals by inhibiting the growth of tumors. Significant inhibition of MH-85 growth in nude mice is observed upon administration of mAb108 i.p. (1 mg/mouse/day) at 1, 5, and 10 days following RG-13022 (400 μg/mouse/day) for 14 days as an MH-85 inoculation.[1]
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| Cell Assay |
The following cell types are plated in complete medium: alpha MEM (100/well; 24-well plate) or HER 14 cells (200/dish; 10-cm dish), with 10% FCS added. The culture medium is changed to either DMEM supplemented with 0.5% PCS and 50 ng/mL EGF (HER14) or alpha MEM supplemented with 0.2% PCS and 50 ng/mL EGF (MH-85) after the overnight culture. For ten days, the cells are cultivated in this medium with or without increasing concentrations of RG-13022. After the culture is complete, the cells are fixed for 15 minutes at room temperature using 4% (v/v) formaldehyde in phosphate-buffered saline that is free of calcium and magnesium, and then they are stained with hematoxylin. Under a microscope, the number of colonies—which contain more than 20 cells in each well—is counted.
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| Animal Protocol |
Mice: MH-85 tumors 5 mm in diameter are injected subcutaneously (s.c.) into the right dorsal region of male BALB/c nu/nu mice that are 4–6 weeks old. I.p. injections of RG-13022 or RG-14620 in 0.1 ml 100% DMSO are given twice a day starting one day following the inoculation of the MH-85 tumor. The vehicle is given to control animals. Under nembutal anesthesia (0.05 mg/g body weight, i.p.), tumor sizes are measured once a week and computed.
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| References |
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| Additional Infomation |
3-(3,4-dimethoxyphenyl)-2-(3-pyridinyl)-2-propenenitrile is a dimethoxybenzene.
RG 13022 is a tyrosine kinase inhibitor that selectively inhibits epidermal growth factor receptor, epidermal factor-stimulated HER14 cell proliferation, and tumor growth in vivo. (NCI) |
| Molecular Formula |
C16H14N2O2
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|---|---|
| Molecular Weight |
266.3
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| Exact Mass |
266.106
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| Elemental Analysis |
C, 72.17; H, 5.30; N, 10.52; O, 12.02
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| CAS # |
136831-48-6
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| Related CAS # |
136831-48-6
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| PubChem CID |
5468216
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| Appearance |
White to off-white solid powder
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| Density |
1.172g/cm3
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| Boiling Point |
423.8ºC at 760mmHg
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| Melting Point |
118 °C
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| Flash Point |
210.1ºC
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| Vapour Pressure |
2.18E-07mmHg at 25°C
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| Index of Refraction |
1.605
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| LogP |
3.162
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
385
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N#C/C(C1=CC=CN=C1)=C/C2=CC=C(OC)C(OC)=C2
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| InChi Key |
DBGZNJVTHYFQJI-ZSOIEALJSA-N
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| InChi Code |
InChI=1S/C16H14N2O2/c1-19-15-6-5-12(9-16(15)20-2)8-14(10-17)13-4-3-7-18-11-13/h3-9,11H,1-2H3/b14-8-
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| Chemical Name |
(E)-3-(3,4-dimethoxyphenyl)-2-pyridin-3-ylprop-2-enenitrile
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| Synonyms |
RG13022; RG-13022; RG 13022; Tyrphostin; RG 13022
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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: ~100 mg/mL (~375.5 mM)
Ethanol: ~5 mg/mL (~18.8 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.39 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
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 (9.39 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. 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 (9.39 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 | 3.7552 mL | 18.7758 mL | 37.5516 mL | |
| 5 mM | 0.7510 mL | 3.7552 mL | 7.5103 mL | |
| 10 mM | 0.3755 mL | 1.8776 mL | 3.7552 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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