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AG-1478 (Synonyms: Tyrphostin AG-1478; NSC 693255) 纯度: 99.22%
AG-1478 (Tyrphostin AG-1478) 是一种选择性的 EGFR 酪氨酸激酶抑制剂,IC50 为 3 nM。AG-1478 对 HCV 和脑心肌炎病毒 (EMCV) 具有抗病毒作用。
AG-1478 Chemical Structure
CAS No. : 153436-53-4
规格 | 价格 | 是否有货 | 数量 |
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥550 | In-stock | |
5 mg | ¥500 | In-stock | |
10 mg | ¥700 | In-stock | |
50 mg | ¥2500 | In-stock | |
100 mg | ¥3500 | In-stock | |
200 mg | 询价 | ||
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AG-1478 相关产品
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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). |
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IC50 & Target |
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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[1]. 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[2]. 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[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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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)[2]. 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[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
315.75 |
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Formula |
C16H14ClN3O2 |
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CAS 号 |
153436-53-4 |
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中文名称 |
酪氨酸磷酸化抑制剂 AG-1478 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 100 mg/mL (316.71 mM) * “≥” means soluble, but saturation unknown. 配制储备液
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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。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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
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参考文献 |
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Cell Assay [1] |
DU145 (HTB-81) and A549 (CCL-185) cells are seeded on 96-well plates at concentrations of 4×103 cells/well in MEM (DU145 cells) or DMEM (A549 cells). Following 24 h of incubation, the culture medium is replaced with serum-free DMEM/F12 (1:1) supplemented with Transferrin (5 mg/mL), sodium selenite (2 ng/mL) and albumin (0.5 mg/mL) [DMEM/F12+]. After an additional 24 h of incubation (Day 0), the medium is replaced by serum-free DMEM/F12+ medium containing tyrosine kinase inhibitors: AG494, AG-1478 respectively in concentration ranges 1-20 μM and 0.1-8 μM. The incubation is continued for the next 24 h at 37°C in a humidified atmosphere. The modified crystal violet staining method (CV) and MTT assay are used to determine the influence of the tyrphostins on the proliferation of target cells. The absorbance is measured using a Tecan multiscan plate recorder[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [2][3] |
Mice[2] 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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