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TYRPHOSTIN B7

CAS No.134036-53-6
Chemical Name:TYRPHOSTIN B7
CBNumber:CB2288901
Molecular Formula:C15H9N5
Formula Weight:259.27
MOL File:134036-53-6.mol

TYRPHOSTIN B7 Property

Boiling point 714.1±60.0 °C(Predicted)
Density 1.396±0.06 g/cm3(Predicted)
storage temp. −20°C
solubility DMSO: soluble
pka 15.95±0.30(Predicted)
form Yellow solid.
color White to yellow

Safety

Safety Statements :22-24/25
WGK Germany :3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Hazard statements
Precautionary statements

TYRPHOSTIN B7 Chemical Properties,Usage,Production

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 selectively inhibit PTKs of key growth factors such as epidermal growth factor (EGF) or platelet-derived growth factor (PDGF) by blocking the phosphorylation of specific tyrosine residues. AG-370 is a selective inhibitor of PDGF receptor kinase with an IC₅₀ value of 20 μM in human bone marrow fibroblasts. It displays comparatively weak inhibition of the EGF receptor (IC₅₀ = 820 μM).
Uses 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].
Definition ChEBI: AG-370 is a member of indoles.
in vitro previous study found that ag-370 inhibited pdgf receptor autophosphorylation and the tyrosine phosphorylation of intracellular protein substrates that coprecipitated with the pdgf receptor in digitonin-permeabilized fibroblasts and in intact fibroblasts. when compared with ag18, a potent egf receptor blocker, ag370 was more efficient in inhibiting pdgf-induced proliferation of fibroblasts and phosphorylation of the intracellular protein substrates. under the conditions in which ag370 could inhibit pdgf-induced mitogenesis and phosphorylation, ag18 did not alter [125i]pdgf internalization and enhance [125i]pdgf binding. these findings suggested that ag370 might have a therapeutic potential for treatment of diseases involving abnormal cellular proliferation induced by pdgf [1].
IC 50 20 μm for pdgf receptor kinase in human bone marrow fibroblasts
References [1] bryckaert, m. c.,eldor, a.,fontenay, m., et al. inhibition of platelet-derived growth factor-induced mitogenesis and tyrosine kinase activity in cultured bone marrow fibroblasts by tyrphostins. experimental cell research 199, 255-261 (1992).