PZ-1

Code: SML1693-5MG D2-231

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 inhibi...


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Your Price
€107.66 5MG
€132.42 inc. VAT

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

assay≥98% (HPLC)
colorwhite to beige
formpowder
Quality Level100
SMILES stringCN1N=CC(C(C=C2)=CC3=C2N(C4=CC=C(CC(NC5=NOC(C(C)(C)C)=C5)=O)C=C4)C=N3)=C1
solubilityDMSO: 1 mg/mL, clear (warmed)
storage temp.2-8°C
Cas Number1800505-64-9
This product has met the following criteria to qualify for the following awards:



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