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AG-370

Names

[ CAS No. ]:
134036-53-6

[ Name ]:
AG-370

[Synonym ]:
(3E)-2-Amino-4-(1H-indol-5-yl)buta-1,3-diene-1,1,3-tricarbonitrile
1,3-Butadiene-1,1,3-tricarbonitrile, 2-amino-4-(1H-indol-5-yl)-, (3Z)-
3-AMINO-4-(1H-INDOL-5-YLMETHYLENE)-2-PENTENETRICARBONITRILE
2-amino-4-(1HA-indol-5-yl)-1,1,3-tricyanobuta-1,3-diene
1,3-Butadiene-1,1,3-tricarbonitrile, 2-amino-4-(1H-indol-5-yl)-, (3E)-
(3E)-2-Amino-4-(1H-indol-5-yl)-1,3-butadiene-1,1,3-tricarbonitrile
2-amino-4-(1H-indol-5-yl)-1,1,3-tricyanobuta-1,3-diene
(3Z)-2-Amino-4-(1H-indol-5-yl)-1,3-butadiene-1,1,3-tricarbonitrile

Biological Activity

[Description]:

AG 370, an indole tyrphostin, is a potent PDGF-induced mitogenesis inhibotor (IC50 of 20 μM). AG 370 displays weak inhibition of the EGF receptor[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR

[Target]

PDGFR:20 μM (IC50)


[In Vitro]

AG 370 blocks mitogenesis induced by epidermal growth factor (IC50 of 50 μM) and human serum (IC50 of 50 μM)[1][1]. In Digitonin-permeabilized fibroblasts as well as in intact fibroblasts, tyrphostin AG 370 inhibits PDGF receptor autophosphorylation and the tyrosine phosphorylation of intracellular protein substrates (pp120, pp85, and pp75) which coprecipitate with the PDGF receptor[1][1].

[References]

[1]. M C Bryckaert, et al. Inhibition of platelet-derived growth factor-induced mitogenesis and tyrosine kinase activity in cultured bone marrow fibroblasts by tyrphostins. Exp Cell Res. 1992 Apr;199(2):255-61.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
714.1±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C15H9N5

[ Molecular Weight ]:
259.266

[ Flash Point ]:
385.7±32.9 °C

[ Exact Mass ]:
259.085785

[ PSA ]:
113.18000

[ LogP ]:
1.39

[ Vapour Pressure ]:
0.0±2.3 mmHg at 25°C

[ Index of Refraction ]:
1.752

Related Compounds