AG-1478|153436-53-4|(Tyrphostin AG-1478; NSC 693255)-陌孚医药/Medlife

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AG-1478 (Synonyms: Tyrphostin AG-1478; NSC 693255)

目录号: PC11646 纯度: ≥98%

CAS No. :153436-53-4

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PC11646-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥490.00	请登录

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中文名称

AG-1478

中文别名

酪氨酸激酶抑制剂AG 1478;N-(3-氯苯基)-6,7-二甲氧基喹唑啉-4-胺;(3-氯苯基)(6,7-二甲氧基喹唑啉-4-基)胺;4-(3-氯苯胺)-6,7-二甲氧基喹唑啉盐酸盐;Tyrphostin AG 1478 酪氨酸激酶抑制剂AG 1478;酪氨酸激酶抑制剂AG;6-羟基嘌呤;次黄嘌呤.6-羟基嘌呤;N-(3-氯苯基)-6,7-二甲氧基-4-氨基喹唑啉;AG-1478, 一种选择性EGFR抑制剂

英文名称

AG-1478

英文别名

4-Quinazolinamine,N-(3-chlorophenyl)-6,7-dimethoxy-;Tyrphostin AG 1478;AG 1478 HYDROCHLORIDE;AG1478;AG-1478;AG-1478 (Tyrphostin AG-1478);N-(3-chlorophenyl)-6,7-dimethoxy-4-Quinazolinamine;N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine;Tyrphostin AG 1478 (AG 1478,NSC-693255);AG-1478 hydrochloride;NSC693255;Tyrphostin;Tyrphostin AG-1478;(3-Chlorophenyl)(6,7-dimethoxyquinazolin-4-yl)amine;AG1478HCl;AG-1478 (NSC-693255);4-(3-CHLOROANILINO)-6,7-DIMETHOXYQUINAZOLINE HCL;NSC 693255;Tyrphostin AG 1478, free base >99%;AG-1478, 97.5%, a selective EGFR inhibitor;4-(3-Chloroanilino)-6,7-dimethoxyquinazoline;AG 1478;4-Quinazolinamine, N-(3-chlorophenyl)-6,7-dimethoxy-;SUH0SEZ9HY;N-(3-chlorophenyl)-6,7-dimethoxy-quinazolin-4-amine;BRD6408;4-(3-Chloroanilino)-6,7-Dimethoxyquinazoline Hydrochloride

Cas No.

153436-53-4

分子式

C₁₆N₃O₂ClH₁₄

分子量

315.75

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

AG-1478 (Tyrphostin AG-1478) is a selective EGFR tyrosine kinase inhibitor with IC₅₀ of 3 nM. AG-1478 has antiviral effects against HCV and encephalomyocarditis virus (EMCV).

性状

Solid

IC50 & Target[1][2]

EGFR

3 nM (IC₅₀)

HCV

EMCV

体外研究(In Vitro)

AG-1478 (AG1478) is irreversible for growth regulation of human lung (A549) and prostate (DU145) cancer cell lines, cultured in chemically defined DMEM/F12 medium. AG-1478 seems to be more effective at lower concentrations, but is unable to completely inhibit growth of A549 cells. Inhibition of EGFR by specific tyrosine kinase inhibitor AG-1478 (AG1478) significantly decreases the angiotensin II-mediated synthesis of TGF-β and fibronectin by cardiac fibroblasts. EGFR is pharmacologically inhibited by small-molecule inhibitor AG-1478 with IC₅₀ of 4 nM. Both Polyfect (PF) and Superfect (SF) treatment lead to increased apoptosis in HEK 293 cells to a similar extent as assessed by flow cytometry. The antioxidant, tempol, significantly reduced dendrimer-mediated apoptosis for both PF and SF. AG-1478 (AG1478), at a 10-fold higher dose (100 μM) than used in signaling studies, is used as a positive control and significantly induced apoptosis in HEK 293 cells.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Administration of AG-1478 (AG1478) significantly reduces myocardial inflammation, fibrosis, apoptosis, and dysfunction in both two obese mouse models. ApoE mice are first fed with HFD for 8 weeks (ApoE-HFD), and then administrated with AG-1478 (10 mg/kg/day) or 542 (10 mg/kg/day) for another 8 weeks by oral gavage. AG-1478 or 542 treatment blocks HFD induced cardiac EGFR phosphorylation in vivo, without affecting the plasma level of low density lipoprotein (LDL) and total triglyceride (TG). Administration of EGF (10 nM) leads to a robust and reproducible elevation in EGFR phosphorylation that can be blocked by AG-1478 (AG1478), a known inhibitor of EGFR phosphorylation. Increasing doses of Polyfect (PF) result in a significant reduction in EGF-induced EGFR phosphorylation (p<0.05) but this is to a lesser extent than observed with AG1478.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Bojko A, et al. The effect of tyrphostins AG494 and AG1478 on the autocrine growth regulation of A549 and DU145 cells. Folia Histochem Cytobiol. 2012 Jul 5;50(2):186-95. [Information]

[2]. Li W, et al. EGFR Inhibition Blocks Palmitic Acid-induced inflammation in cardiomyocytes and Prevents Hyperlipidemia-induced Cardiac Injury in Mice. Sci Rep. 2016 Apr 18;6:24580. [Information]

[3]. Akhtar S, et al. Cationic Polyamidoamine Dendrimers as Modulators of EGFR Signaling 体外研究 and In Vivo. PLoS One. 2015 Jul 13;10(7):e0132215. [Information]

[4]. Dorobantu CM, et al. Tyrphostin AG1478 Inhibits Encephalomyocarditis Virus and Hepatitis C Virus by Targeting Phosphatidylinositol 4-Kinase IIIα. Antimicrob Agents Chemother. 2016 Sep 23;60(10):6402-6. [Information]

溶解度数据

体外研究:

DMSO : 50 mg/mL (158.35 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 1% CMC 0.5% Tween-80
Solubility: 5 mg/mL (15.84 mM); Suspended solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (6.59 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.59 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (6.59 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.59 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.59 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.59 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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