ChemicalBook > CAS DataBase List > AG 1478 HYDROCHLORIDE

AG 1478 HYDROCHLORIDE

CAS No.153436-53-4
Chemical Name:AG 1478 HYDROCHLORIDE
CBNumber:CB4728982
Molecular Formula:C16H14ClN3O2
Formula Weight:315.75
MOL File:153436-53-4.mol

AG 1478 HYDROCHLORIDE Property

Melting point 247 °C(dec.)
Boiling point 458.5±45.0 °C(Predicted)
Density 1.337
storage temp. Keep in dark place,Inert atmosphere,2-8°C
solubility insoluble in H2O; ≥15.8 mg/mL in DMSO; ≥2.38 mg/mL in EtOH with gentle warming
pka 5.54±0.30(Predicted)
form White to light yellow solid.
color Light orange to Yellow to Green
λmax 332nm(lit.)
FDA UNII SUH0SEZ9HY

Safety

RTECS :VA0953000
HS Code :29339900

NFPA 704:

	0
2		0

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal wordWarning
Hazard statements H302-H315-H319-H332-H335
Precautionary statements P280-P305+P351+P338-P310

AG 1478 HYDROCHLORIDE Price More Price(1)

Brand: TCI Chemicals (India)
Product number: T2944
Product name : Tyrphostin AG 1478
Purity:
Packaging: 25MG
Price: ₹17100
Updated: 2022/05/26
Buy: Buy

AG 1478 HYDROCHLORIDE Chemical Properties,Usage,Production

Uses A highly potent and specific EGFR tyrosine kinase inhibitor with an IC50 of 3 nM.
Uses AG 1478 Hydrochloride is an epidermal growth factor receptor tyrosine kinase inhibior (EGFR inhibtor).
Definition ChEBI: Tyrphostin AG 1478 is a member of the class of quinazolines that is quinazoline substituted by methoxy groups at positions 6 and 7 and a (3-chlorophenyl)nitrilo group at position 4. It acts as an epidermal growth factor receptor antagonist. It has a role as an epidermal growth factor receptor antagonist, an antineoplastic agent, a geroprotector and an antiviral agent. It is a member of quinazolines, an aromatic ether and a member of monochlorobenzenes.
Biological Activity Potent and selective inhibitor of epidermal growth factor receptor kinase (IC 50 values 3 nM for EGFR and > 100 μ M for ErbB2 and PDGFR). Inhibits proliferation of NCI-H2170 NSCLC cells in vitro (IC 50 = 1 μ M).
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].
target EGFR
IC 50 EGFR: 3 nM (IC₅₀); HCV; EMCV