Pz-1
SIGMA/SML1693 - ≥98% (HPLC)
Synonym: N-
CAS Number: 1800505-64-9
Empirical Formula (Hill Notation): C26H26N6O2
Molecular Weight: 454.52
Linear Formula: C26H26N6O2
Product Type: Chemical
| assay | ≥98% (HPLC) |
| color | white to beige |
| form | powder |
| InChI | 1S/C26H26N6O2/c1-26(2,3)2 |
| InChI key | NJLMIILZNLZZFW-UHFFFAOYSA |
| Quality Level | 100  |
| SMILES string | CN1N=CC(C(C=C2)=CC3=C2N(C |
| solubility | DMSO: 1 mg/mL, clear (warmed) |
| storage temp. | 2-8°C |
| 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. |
| Biochem/physiol Actions: | Pz-1 is a cell-permeable, non-cytotoxic and highly potent type II kinase inhibitor that potently inhibits RET and VEGFR2 tyrosine kinase activity. |
| Packaging: | 5, 25 mg in glass bottle |
| RIDADR | NONH for all modes of transport |
| WGK Germany | WGK 3 |
| Flash Point(F) | Not applicable |
| Flash Point(C) | Not applicable |
| Purity | ≥98% (HPLC) |
| Storage Temp. | 2-8°C |
| UNSPSC | 12352200 |