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AG-1478

AG-1478

Item no.	S2728-25
Manufacturer	Selleckchem
CASRN	153436-53-4,175178-82-2
Amount	25 mg
Quantity options	10 mg 1 g 10 g 10 mM/1 mL 25 mg 5 mg 50 mg 5 g
Category	Oncology Neuroscience Neural Lineage Markers Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Bladder Cancer Colorectal Cancer Breast Cancer
Type	Inhibitors
Specific against	other
Smiles	COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Cl)OC
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	Tyrphostin AG-1478,NSC 693255
Similar products	AG-1478, 153436-53-4
Available
Manufacturer - Targets	EGFR
Storage Conditions	2 years -80 in solvent
Molecular Weight	315, 75
Administration	Injection i.p. three times per week
Animal Models	Female BALB/c nu/nu mice inoculated s.c. with A431 or U87MG.delta2-7 tumor cells
Cell lines	U87MG
Concentrations	Dissolved in DMSO, final concentrations ca.100 uM
Dosages	ca.1 mg/kg
Formulation	Dissolved in 100 mM Captisol
IC50	3 nM [1], 3 nM [1], 3 nM [1], 3 nM [1], 3 nM [1], 3 nM [1]
In vitro	AG-1478 is high selective over ErbB2 and PDGFR with IC50 of >100 uM. [1] AG-1478 preferentially inhibits U87MG cells expressing truncated EGFR with IC50 of 8.7 uM, compared to those expressing endogenous wt EGFR or overexpressing exogenous wt EGFR with IC50 of 34.6 uM and 48.4 uM, respectively, and inhibits the DNA synthesis with IC50 of 4.6 uM, 19.67 uM, and 35.2 uM, respectively. AG-1478 also preferentially inhibits the tyrosine kinase activity and autophosphorylation of the deltaEGFR compared to endogenous or overexpressed exogenous wt EGFR. [2] AG-1478 (0.25 uM) 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 uM and 0.2 uM, 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]
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 uCi 90Y-CHX-A''-DTPA-hu3S193 results in a significant enhancement of efficacy compared with either agent alone. [5]
Incubation Time	72 hours
Method	Cells are exposed to different concentrations of AG-1478 for 72 hours in 96-well plates. The effects of AG-1478 on cell growth are examined using an Alamar Blue assay. A 20-L aliquot of Alamar Blue is added to each well, and its absorbance is determined using a Spectromax Scanning Micro plate Reader. The effects of AG-1478 are expressed as percentage of growth inhibition using untreated cells as the control (0% inhibition). Cellular DNA synthesis is determined using a [3H]thymidine incorporation assay.
Solubility (25C)	DMSO 25 mg/mL, Water <1 mg/mL, Ethanol 13 mg/mL
Information	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 (Tyrphostin AG-1478) inhibits encephalomyocarditis virus (EMCV) and hepatitis c virus (HCV) by targeting phosphatidylinositol 4-kinase IIIα (PI4KA).
Chemical Name	N-(3-chlorophenyl)-6, 7-dimethoxyquinazolin-4-amine

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S2728-25-datasheet.pdf

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