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AG-1478

(CAS No:153436-53-4)
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.
CAS No:153436-53-4
Molecular Weight(MW):315.75
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
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QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 153436-53-4
Molecular formula(MF) C16H14ClN3O2
Molecular Weight(MW): 315.75
Alias
Solubility
In vitro DMSO 25 mg/mL (79.17 mM)
Ethanol 13 mg/mL (41.17 mM)
Water <1 mg/mL
In vivo 15% Captisol 30 mg/mL
Biological Activity
Description 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.
Targets
EGFR [1]
(Cell-free assay)		 HER2 [1]
(Cell-free assay)		 PDGFR [1]
(Cell-free assay)
3 nM >100 μM >100 μM
In vitro

AG-1478 is high selective over ErbB2 and PDGFR with IC50 of >100 μM. [1] AG-1478 preferentially inhibits U87MG cells expressing truncated EGFR with IC50 of 8.7 μM, compared to those expressing endogenous wt EGFR or overexpressing exogenous wt EGFR with IC50 of 34.6 μM and 48.4 μM, respectively, and inhibits the DNA synthesis with IC50 of 4.6 μM, 19.67 μM, and 35.2 μM, respectively. AG-1478 also preferentially inhibits the tyrosine kinase activity and autophosphorylation of the ΔEGFR compared to endogenous or overexpressed exogenous wt EGFR. [2] AG-1478 (0.25 μM) abolishes the MAPK activation induced by Ang II, a Ca2+ ionophore as well as EGF but not by a phorbol ester or platelet-derived growth factor-BB in the VSMC. [3] AG-1478 inhibits EGF-induced mitogenesis of the BaF/ERX and LIM1215 cells with IC50 of 0.07 μM and 0.2 μM, respectively. [6] AG1478 is able to inhibit the function of ATP-binding cassette (ABC) transporters such as ABCB1 and ABCG2, with a more pronounced effect on ABCG2. [7]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U87MG Growth inhibitory assay ~100 μM DMSO IC50=34.6 μM 8752145
U87MG.ΔEGFR Growth inhibitory assay ~100 μM DMSO IC50=8.7 μM 8752145
U87MG.wtEGFR. Growth inhibitory assay ~100 μM DMSO IC50=48.4 μM 8752145
U87MG Kinase assay ~100 μM DMSO inhibits EGFR tyrosine kinase activity 8752145
U87MG.ΔEGFR Kinase assay ~100 μM DMSO inhibits EGFR tyrosine kinase activity 8752145
U87MG.wtEGFR. Kinase assay ~100 μM DMSO inhibits EGFR tyrosine kinase activity 8752145
HPV 16-immortalized human keratinocytes Growth inhibitory assay ~50 μM DMSO inhibits cell growth 9288782
HPV 16-immortalized human keratinocytes Function assay ~50 μM DMSO induces arrest in the Cell Cycle 9288782
HPV 16-immortalized human keratinocytes Apoptosis assay ~50 μM DMSO induces apoptosis. 9288782
A431 Kinase assay ~10 μM DMSO inhibits the basal and TGF-α-stimulated tyrosine phosphorylation of the EGFR 10702262
MDA-468  Kinase assay ~10 μM DMSO inhibits the basal and TGF-α-stimulated tyrosine phosphorylation of the EGFR 10702262
A431 Function assay ~10 μM DMSO induces cell cycle arrest 10702262
MDA-MB-231 Kinase assay ~5 μM DMSO inhibits EGF stimulated phosphorylation of FKHR 11030146
CNE2 Growth inhibitory assay 100 μM DMSO inhibits cell proliferation by 98.4% 11410322
CNE2 Kinase assay ~100 μM DMSO inhibits EGFR tyrosine phosphorylation 11410322
CNE2 Function assay ~100 μM DMSO Inhibits MAPK and AKT activation 11410322
CNE2 Function assay ~50 μM DMSO affects cell cycle distribution 11410322
HSC-2 Kinase assay 8 μM DMSO inhibits phosphorylation of EGFR and Akt 17689285
HSC-2 Apoptosis assay 8 μM DMSO inhibits Fas-mediated apoptosis 17689285
HEp-2 Growth inhibitory assay ~10 μM DMSO enhances oridonin-induced growth-inhibitory 20202741
SubG1 Apoptosis assay ~10 μM DMSO enhances oridonin-induced apoptosis 20202741
HEp-2 Function assay ~10 μM DMSO enhances Oridonin-induced Bax activation, Bcl-2 degradation and SIRT1 inactivation 20202741
H508 Growth inhibitory assay ~1 μM DMSO mitigates CPF-mediated H508 cell growth 26514924

... Click to View More Cell Line Experimental Data
In vivo Administration of AG-1478 blocks phosphorylation of the EGFR at the tumor site and inhibits the growth of A431 xenografts that overexpress the WT EGFR and glioma xenografts expressing the de2-7 EGFR. Even subtherapeutic doses of AG-1478 significantly enhance the efficacy of cytotoxic drugs, with the combination of AG-1478 and temozolomide displaying synergistic antitumor activity against human glioma xenografts. The combination of AG-1478 and an anti-EGFR antibody (mAb 806) displays additive and in some cases synergistic, antitumor activity against tumor xenografts overexpressing the EGFR. [4] The combination of AG-1478 (0.4 mg) with a single dose of 25 μCi 90Y-CHX-A''-DTPA-hu3S193 results in a significant enhancement of efficacy compared with either agent alone. [5]
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