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AG-1478

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Category Influenza Virus
CAS 153436-53-4
Description AG-1478 (NSC 693255) is a selective EGFR inhibitor with IC50 of 3 nM; almost no activity on HER2-Neu, PDGFR, Trk, Bcr-Abl and InsR.
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Product Information

Synonyms Tyrphostin AG-1478; AG-1478; AG1478; AG 1478
IUPAC Name N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine
Molecular Weight 315.75
Molecular Formula C16H14ClN3O2
Canonical SMILES COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Cl)OC
InChI InChI=1S/C16H14ClN3O2/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11/h3-9H,1-2H3,(H,18,19,20)
InChIKey GFNNBHLJANVSQV-UHFFFAOYSA-N
Boiling Point 458.5±45.0 °C at 760 mmHg
Melting Point 247 °C(dec.)
Flash Point 231.1±28.7 °C
Purity >98%
Density 1.3±0.1 g/cm3
Solubility In Vitro:
DMSO : 50mg/mL(158.35mM;Need ultrasonic)
In Vivo:
1.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
2.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
3.Add each solvent one by one:10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.59 mM); Clear solution
4.Add each solvent one by one:1% CMC0.5%Tween-80
Solubility: 5 mg/mL (15.84 mM); Suspended solution; Need ultrasonic
Appearance White to off-white (Solid)
Application Enzyme Inhibitors
Storage Powder:
-20°C: 3 years
4°C: 2 years
In solvent:
-80°C: 6 months
-20°C: 1 month
Animal Admin 28 C57BL/6 or ApoE-/- mice are randomly divided into four weight-matched groups. From week 9, AG-1478 or 542 is administered daily by oral gavage at a dose of 10 mg / kg / day for the next 8 weeks. AG-1478 and dendritic polymer treatment are administered at a single dose for 24 h before execution. An automated blood glucose analyzer is used to assess blood glucose concentrations, and rats with blood glucose concentrations above 250 mg/dL (approximately 14 mM) have been declared diabetic.
Assay DU145 (HTB-81) and A549 (CCL-185) cells are seeded in MEM (DU145 cells) or DMEM (A549 cells) on a 96-well plate, supplemented with 100 IU/mL penicillin in the presence of 10% FBS, 100 μg/mL streptomycin. AG494, AG-1478, concentration ranges of 1-20 μM and 0.1-8 μM, respectively. Modified crystal violet staining (CV) and MTT methods were used to determine the effect of tyrphostins on target cell proliferation.
Complexity 360
Exact Mass 315.077454
Index Of Refraction 1.668
In Vitro AG-1478 (AG1478) is irreversible for the growth regulation of human lung (A549) and prostate (DU145) cancer cell lines. Inhibition of EGFR by the specific tyrosine kinase inhibitor AG-1478 (AG1478) significantly reduces the synthesis of TGF-β and fibronectin by angiotensin-II-mediated cardiac fibroblasts.
In Vivo The administration of AG-1478 (AG1478) significantly reduced myocardial inflammation, fibrosis, Apoptosis, and dysfunction in two obese mouse models.
PSA 56.27000
Target EGFR; HCV; Influenza Virus
Vapor Pressure 0.0±1.1 mmHg at 25°C
XLogP3-AA 4

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