AG-1478
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AG-1478 is an inhibitor of EGFR which acts on EGF-stimulated Erk1/2 phosphorylation with IC50 value of 10 uM using ovarian cell line Ishikawa [1].
EGFR (epidermal growth factor receptor) belongs to human HER-1 family, which is a cell surface receptor and recognized by EGF-family (epidermal growth factor family). Many studies have shown that EGFR is over-expressed in a variety of solid tumors and its over-expression means bad prognosis for cancer patients [1]. AG1478 works as EGFR kinase inhibitor through blocking EGFR phosphorylation and superoxide anion production [2].
Treating human hepatocellular carcinoma HA22T/VGH cells could reduce its anti-tumor activity compared with control group [3]. When tested with ovarian cancer cell lines CAOV-3 or SKOV-3, EGFR signaling was diminished [4]. When human colorectal SW480 was treated with AG-1478, both EGFR phosphorylation and cell proliferation were reduced [5].
In nu/nu mice model with CAOV-3 cells xenografted, treatment with AG-1478 could diminish EGFR phosphorylation thus limited the growth of tumor [4].
Gong XD, et al. had shown that AG-1478 also could reduce the expression of FOXM1 via FOXO3a using a NSCLC cell lines A549, and the A549 cells showed increased chemosensitivity[6].
References:
1.Takai, N., et al., Synergistic anti-neoplastic effect of AG1478 in combination with cisplatin or paclitaxel on human endometrial and ovarian cancer cells. Mol Med Rep, 2010. 3(3): p. 479-84.
2.D'Anneo, A., et al., Parthenolide induces superoxide anion production by stimulating EGF receptor in MDA-MB-231 breast cancer cells. Int J Oncol, 2013. 43(6): p. 1895-900.
3.Bondi, M.L., et al., Entrapment of an EGFR inhibitor into nanostructured lipid carriers (NLC) improves its antitumor activity against human hepatocarcinoma cells. J Nanobiotechnology, 2014. 12(21): p. 1477-3155.
4.Yu, Y., et al., Synergistic effects of combined platelet-activating factor receptor and epidermal growth factor receptor targeting in ovarian cancer cells. J Hematol Oncol, 2014. 7(1): p. 1756-8722.
5.Yagublu, V., et al., Combination of the EGFR tyrosine kinase inhibitor AG1478 and 5-FU: no synergistic effect on EGFR phosphorylation, cell proliferation and apoptosis induction. Anticancer Res, 2013. 33(9): p. 3753-8.
6.Gong, X.D., et al., [Effects of AG1478 on the expression of FOXM1 gene via FOXO3a in non-small cell lung cancer cells]. Zhonghua Zhong Liu Za Zhi, 2013. 35(8): p. 572-8.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 315.75 |
| Cas No. | 153436-53-4 |
| Formula | C16H14ClN3O2 |
| Synonyms | Tyrphostin AG-1478; AG 1478; NSC 693255; AG1478 |
| Solubility | ≥15.8mg/mL in DMSO |
| Chemical Name | N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine |
| SDF | Download SDF |
| Canonical SMILES | COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Cl)OC |
| Shipping Condition | Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request. |
| General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months. |
| Cell experiment [1]: | |
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Cell lines |
Human hepatocellular carcinoma HA22T/VGH cell line |
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Preparation method |
Soluble in DMSO > 15.8mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
6.25, 12.5, 25μM; 24hr |
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Applications |
Tyrphostin AG-1478, a potent and specific inhibitor of EGFR (Epidermal Growth Factor Receptor) tyrosine kinase, plays a key role in the control of normal cellular growth and abnormal cell proliferation. Tyrphostin AG-1478 shows an enhanced in vitro anti-tumor activity in HA22T/VGH cells when entrapmented into NLC(nanostructured lipid carriers) systems compared to free drug. |
| Animal experiment [2]: | |
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Animal models |
Male C57BL/6 mice aged 8 weeks, male ApoE-/- mice aged 8 weeks |
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Dosage form |
10 mg/kg/day, 8 weeks, oral gavage |
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Application |
Administration of AG1478 significantly reduced myocardial inflammation, fibrosis, apoptosis, and dysfunction in both two obese mouse models. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Bondì ML1, Azzolina A, et al, Entrapment of an EGFR inhibitor into nanostructured lipid carriers (NLC) improves its antitumor activity against human hepatocarcinoma cells. J Nanobiotechnology, 2014. 12(21): p. 1477-3155. [2]. Li W1,2, Fang Q1, EGFR Inhibition Blocks Palmitic Acid-induced inflammation in cardiomyocytes and Prevents Hyperlipidemia-induced Cardiac Injury in Mice. Sci Rep. 2016 Apr 18;6:24580. doi: 10.1038/srep24580. | |
| Description | AG-1478 (Tyrphostin AG-1478) is a selective inhibitor of EGFR with an IC50 values of 3 nM. | |||||
| Targets | EGFR | HER2 | PDGFR | |||
| IC50 | 3 nM | >100 μM | >100 μM | |||
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