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AG-1478

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Category Hepatitis C Virus (HCV)
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.
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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