AG-1478

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AG-1478 (Tyrphostin AG-1478) 是一种选择性 EGFR 抑制剂，在无细胞试验中 IC50 为 3 nM，对 HER2-Neu、PDGFR、Trk、Bcr-Abl 和 InsR 几乎没有活性。

AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor with IC50 of 3 nM in cell-free assays, almost no activity on HER2-Neu, PDGFR, Trk, Bcr-Abl and InsR.

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.

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.

NSC 693255 | Tyrphostin AG-1478

Angiogenesis

EGFR

EGFR| HER2| PDGFR

Cancer

——

153436-53-4

315.75

C16H14ClN3O2

>98% (HPLC)

Ethanol: 13 mg/mL (41.17 mM); DMSO: 25 mg/mL (79.17 mM)

COC1=CC2=NC=NC(NC3=CC=CC(Cl)=C3)=C2C=C1OC

N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine

(-20℃)

With Ice Pack

≥ 2 years