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ChemicalBook--->CAS DataBase List--->146535-11-7

146535-11-7

146535-11-7 Structure

146535-11-7 Structure
IdentificationBack Directory
[Name]

TYRPHOSTIN AG 1296
[CAS]

146535-11-7
[Synonyms]

1296
AG 1296
AG-1296;AG 1296;
TYRPHOSTIN AG 1296
TYRPHOSTIN AG 1296 USP/EP/BP
Tyrphostin AG 1296 (AG 1296)
AG-1296 (Tyrphostin AG 1296)
6,7-DIMETHOXY-2-PHENYLQUINOXALINE
6,7-DIMETHOXY-3-PHENYLQUINOXALINE
Quinoxaline,6,7-dimethoxy-2-phenyl-
AG 1296 - CAS 146535-11-7 - Calbiochem
[Molecular Formula]

C16H14N2O2
[MDL Number]

MFCD00270913
[MOL File]

146535-11-7.mol
[Molecular Weight]

266.29
Chemical PropertiesBack Directory
[Boiling point ]

420.2±40.0 °C(Predicted)
[density ]

1.192±0.06 g/cm3(Predicted)
[storage temp. ]

2-8°C
[solubility ]

Soluble in DMSO.
[form ]

White solid
[pka]

0.48±0.30(Predicted)
[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 DataBack Directory
[WGK Germany ]

3
Hazard InformationBack Directory
[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.
[Uses]

A potent inhibitor of PDGF receptor tyrosine kinase (IC50=1 μM). Also inhibits FGF receptor tyrosine kinase and c-kit. Induces apoptosis in a small-cell lung cancer cell line (H526).
[Definition]

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

PDGFR
[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
Spectrum DetailBack Directory
[Spectrum Detail]

TYRPHOSTIN AG 1296(146535-11-7)1HNMR
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