PZ-1

Stock Code: 3575277
Manufacturer Part No: SML1693-5MG

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Descriptions

Biochem/physiol Actions

Pz-1 is a cell-permeable, non-cytotoxic (up to 0.1 µM and 6 days; NIH/3T3 cells), and highly potent type II kinase inhibitor that potently inhibits RET and VEGFR2 tyrosine kinase activity (IC₅₀ ﹤1 nM; [ATP] = 190 µM) by targeting the kinases in their inactive DFG-out conformation, displaying significant affinity (Kd ﹤50 nM) toward only TRKB, TRKC, GKA, FYN, SRC, TAK1, MUSK from a panel of 96 other kinases. Pz-1 inhibits cellular RET mutants (C634R, C634Y, V804L, V804M, M918T) and VEGFR2 phosphorylations, and selectively inhibits the growth of RET C634Y- than HRas G12V-transformed NIH/3T3 cultures (IC₅₀= 0.5 vs. 34.4 nM). Likewise, Pz-1 completely abrogated tumor formation from RET C634Y-transformed NIH/3T3 cells in mice in vivo (1 mg/kg/d, p.o.), while only up to 70% tumor suppression of HRas G12V-transformed cells was achieved with 10 mg/kg daily oral dosage.

Packaging

5, 25 mg in glass bottle