TYRPHOSTIN AG 1296

Synonym(s):6,7-Dimethoxy-3-phenylquinoxaline;AG 1296 - CAS 146535-11-7 - Calbiochem

CAS NO.：146535-11-7
Empirical Formula: C16H14N2O2
Molecular Weight: 266.29
MDL number: MFCD00270913
SAFETY DATA SHEET (SDS)
Update Date: 2026-03-13 23:13:44

What is TYRPHOSTIN AG 1296?

Description

Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors specific for platelet-derived growth factor (PDGF) receptor kinase could help in the treatment of atherosclerosis, restenosis, pulmonary fibrosis, and gliomas. AG-1296 is a potent and selective inhibitor of PDGF receptor kinase with an IC₅₀ value of about 0.4 μM both in vitro and in cells (Swiss 3T3 cells). It inhibits ligand-stimulated DNA synthesis in platelet-derived growth factor receptor and stem cell factor/kit receptor transfected cells with an IC₅₀ values of 1.5 and 1.8 μM, respectively. Treatment of sis oncogene transfected NIH3T3 cells with AG-1296 reverses the transformed phenotype.

The Uses of TYRPHOSTIN AG 1296

Tyrphostin AG 1296, is the platelet-derived growth factor receptor (PDGFR) inhibitor, which can causes growth inhibition in glioblastoma cells.

What are the applications of Application

AG-1296 is a potent inhibitor of PDGFR kinase and c-Kit

Definition

ChEBI: 6,7-dimethoxy-2-phenylquinoxaline is a quinoxaline derivative.

References

1) Kovalenko et al. (1997), Phosphorylation site-specific inhibition of platelet-derived growth factor beta-receptor autophosphorylation by the receptor blocking tyrphostin AG1296; Biochemistry, 36 6260 2) Krystal et al. (1997), Induction of apoptosis and inhibition of small cell lung cancer growth by the quinoxaline tyrphostins; Cancer Res., 57 220 3) Strutz et al. (2001), TGF-beta 1 induces proliferation in human renal fibroblasts via induction of basic fibroblast growth factor (FGF-2); Kidney Int., 59 579

Properties of TYRPHOSTIN AG 1296

Boiling point:	420.2±40.0 °C(Predicted)
Density	1.192±0.06 g/cm3(Predicted)
storage temp.	Keep in dark place,Sealed in dry,Store in freezer, under -20°C
solubility	Soluble in DMSO.
pka	0.48±0.30(Predicted)
form	White solid
color	Yellow
Sensitive	Light Sensitive
Stability:	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Safety information for TYRPHOSTIN AG 1296

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes	P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.