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AG-1478 Sale

(Synonyms: Tyrphostin AG-1478; AG 1478; NSC 693255; AG1478) 目录号 : GC17226

An inhibitor of EGF receptor kinase

AG-1478 Chemical Structure

Cas No.:153436-53-4

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥378.00
现货
5mg
¥368.00
现货
25mg
¥1,092.00
现货
50mg
¥1,932.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

Human hepatocellular carcinoma HA22T/VGH cell line

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.

Reacting condition

6.25, 12.5, 25μM; 24hr

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]:

Animal models

Male C57BL/6 mice aged 8 weeks, male ApoE-/- mice aged 8 weeks

Dosage form

10 mg/kg/day, 8 weeks, oral gavage

Application

Administration of AG1478 significantly reduced myocardial inflammation, fibrosis, apoptosis, and dysfunction in both two obese mouse models.

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.

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.

产品描述

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.

Chemical Properties

Cas No. 153436-53-4 SDF
别名 Tyrphostin AG-1478; AG 1478; NSC 693255; AG1478
化学名 N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine
Canonical SMILES COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Cl)OC
分子式 C16H14ClN3O2 分子量 315.75
溶解度 ≥ 15.8mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.1671 mL 15.8353 mL 31.6706 mL
5 mM 0.6334 mL 3.1671 mL 6.3341 mL
10 mM 0.3167 mL 1.5835 mL 3.1671 mL
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