SML1693

Pz-1

≥98% (HPLC)

• Sinonimo/i: N-(5-(Tert-Butyl)isoxazol-3-yl)-2-(4-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)phenyl)acetamide
• Formula empirica (notazione di Hill): C₂₆H₂₆N₆O₂
• Numero CAS: 1800505-64-9
• Peso molecolare: 454.52
• Codice UNSPSC: 12352200
• ID PubChem: 329826021
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥98% (HPLC)
• Stato: powder
• Colore: white to beige
• Solubilità: DMSO: 1 mg/mL, clear (warmed)
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: CN1N=CC(C(C=C2)=CC3=C2N(C4=CC=C(CC(NC5=NOC(C(C)(C)C)=C5)=O)C=C4)C=N3)=C1
• InChI: 1S/C26H26N6O2/c1-26(2,3)23-13-24(30-34-23)29-25(33)11-17-5-8-20(9-6-17)32-16-27-21-12-18(7-10-22(21)32)19-14-28-31(4)15-19/h5-10,12-16H,11H2,1-4H3,(H,29,30,33); NJLMIILZNLZZFW-UHFFFAOYSA-N

Descrizione

Azioni biochim/fisiol

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.

Pz-1 is a cell-permeable, non-cytotoxic and highly potent type II kinase inhibitor that potently inhibits RET and VEGFR2 tyrosine kinase activity.

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable