[CAS NO. 153436-53-4] AG-1478

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PRODUCTS SPECIFICATIONS [153436-53-4]

Catalog

HY-13524

Brand

MCE

CAS

153436-53-4

DESCRIPTION [153436-53-4]

Overview

MDL	MFCD00270914
Molecular Weight	315.75
Molecular Formula	C16H14ClN3O2
SMILES	COC1=CC2=NC=NC(NC3=CC=CC(Cl)=C3)=C2C=C1OC

For research use only. We do not sell to patients.

27 Publications Citing Use of MCE

Summary

AG-1478 (Tyrphostin AG-1478) is a selective EGFR tyrosine kinase inhibitor with IC ₅₀ of 3 nM. AG-1478 has antiviral effects against HCV and encephalomyocarditis virus (EMCV) .

IC50 & Target

EGFR

3 nM (IC ₅₀ )

HCV

EMCV

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 IC ₅₀ 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] .

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

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] .

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

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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

Preparing
Stock Solutions

Concentration Solvent Mass	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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 1% CMC >> 0.5% Tween-80

Solubility: 5 mg/mL (15.84 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (6.59 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (6.59 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (6.59 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

4-Quinazolinamine, N-(3-chlorophenyl)-6,7-dimethoxy-

N-(3-Chlorophenyl)-6,7-dimethoxy-4-quinazolinamine

AG 1478

Tyrphostin AG 1478

NSC 693255

(3-Chlorophenyl)(6,7-dimethoxyquinazolin-4-yl)amine

BRD-K68336408