AG-18 (Synonyms: RG50810, RG50858, TX 825, Tyrphostin 23, Tyrphostin AG18) |
| カタログ番号GC17647 |
AG-18 (Tyrphostin A23) は、それぞれ IC50 と Kiof 35 および 11 μM を持つ EGFR 阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 118409-57-7
Sample solution is provided at 25 µL, 10mM.
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AG18 is an inhibitor of EGFR kinase with IC50 values of 35μM. [3]
AG18 acts as general tyrosine kinase inhibitor to block tyrosine phosphorylation and events downstream of tyrosine phosphorylation. [1]
AG18 and AG10 reduced cellular ATP by 90% and increased the rate of oxygen consumption in the absence of the muscarinic agonist carbachol, indicating that these tyrphostins uncouple mitochondria. AG18 and AG10 blocked parotid phosphorylation events only at concentrations that reduced ATP content. AG18 and AG10 also activated AMPK and/or uncoupled mitochondria inHEK293, PC12, and HeLa cells. [1]
In granulosa-lutein cells, tyrphostin AG18 reversiblely arrested the FSH-induced accumulation of P450scc mRNA with IC50 value of 15 mu M. However, AG18 did not accelerate the mRNA degradation process. Moreover, even the extremely high levels of P450scc mRNA in granulosa-lutein cells, were not affected by the addition of AG18 in culture. Aromatase cytochrome P450 and 3 beta-hydroxysteroid dehydrogenase-I, were inhibited by AG18 at their mRNA levels. [2]
References:
[1]. Soltoff SP. Evidence that tyrphostins AG10 and AG18 are mitochondrial uncouplers that alter phosphorylation-dependent cell signaling. J Biol Chem. 2004 Mar 19;279(12):10910-8. Epub 2003 Dec 19.
[2]. Orly J, Rei Z, Greenberg NM et al. Tyrosine kinase inhibitor AG18 arrests follicle-stimulating hormone-induced granulosa cell differentiation: use of reverse transcriptase-polymerase chain reaction assay for multiple messenger ribonucleic acids. Endocrinology. 1994 Jun;134(6):2336-46.
[3]. Gazit A, Yaish P, Gilon C et al. Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors. J Med Chem. 1989 Oct;32(10):2344-52.
| Cas No. | 118409-57-7 | SDF | |
| 同義語 | RG50810, RG50858, TX 825, Tyrphostin 23, Tyrphostin AG18 | ||
| Chemical Name | 2-[(3,4-dihydroxyphenyl)methylidene]propanedinitrile | ||
| Canonical SMILES | C1=CC(=C(C=C1C=C(C#N)C#N)O)O | ||
| Formula | C10H6N2O2 | M.Wt | 186.17 |
| 溶解度 | ≥ 9.3mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 5.3714 mL | 26.8572 mL | 53.7143 mL |
| 5 mM | 1.0743 mL | 5.3714 mL | 10.7429 mL |
| 10 mM | 0.5371 mL | 2.6857 mL | 5.3714 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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