SU 16f

Uses

SU 16f is used in the synthetic preparation of [(Dihydrooxoindolylidene)methyl]pyrrolepropanoic Acid as a tyrosine kinase inhibitor.

General Description

A cell-permeable indolinone compound that acts as a potent, ATP site-targeting PDGFR inhibitor (IC₅₀ = 10 nM against PDGFRβ), while affecting Flk-1/KDR/ VEGFR2, FGFR1, and EGFR only at much higher concentrations (IC₅₀ = 0.14, 2.29, and >100 μM, respectively). Reported to selectively inhibit PDGFβ- over EGF-stimulated proliferation in EGFR-expressing NIH 3T3 cultures (IC₅₀ = 0.11 and 21.9 μM, respectively) and exhibit much weaker potency against the proliferation of HUVEC cells upon FGF or VEGF stimulation (IC₅₀ = 10 μM).

IC 50

PDGFRβ: 10 nM (IC₅₀); PDGFR2: 140 nM (IC₅₀); PDGFR1: 2.29 μM (IC₅₀)

storage

Store at RT