PZ-1
- Product Name
- PZ-1
- CAS No.
- 1800505-64-9
- Chemical Name
- PZ-1
- Synonyms
- PZ-1;Pz-1 >=98% (HPLC);Pz-1, 10 mM in DMSO;Pz 1,Vascular endothelial growth factor receptor,inhibit,RET,Pz-1,VEGFR,Inhibitor,Pz1;N-(5-(tert-Butyl)isoxazol-3-yl)-2-(4-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)phenyl)acetamide;Benzeneacetamide, N-[5-(1,1-dimethylethyl)-3-isoxazolyl]-4-[5-(1-methyl-1H-pyrazol-4-yl)-1H-benzimidazol-1-yl]-;N-(5-(tert-Butyl)isoxazol-3-yl)-2-(4-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)phenyl)acetamide , Pz-1
- CBNumber
- CB64741125
- Molecular Formula
- C26H26N6O2
- Formula Weight
- 454.52
- MOL File
- 1800505-64-9.mol
PZ-1 Property
- Density
- 1.28±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- Soluble in DMSO
- form
- powder
- pka
- 12?+-.0.70(Predicted)
- color
- white to beige
N-Bromosuccinimide Price
- Product number
- SML1693
- Product name
- Pz-1
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $108
- Updated
- 2024/03/01
- Product number
- SML1693
- Product name
- Pz-1
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $386
- Updated
- 2022/05/15
- Product number
- CS-0035381
- Product name
- Pz-1
- Purity
- >99.0%
- Packaging
- 10mg
- Price
- $390
- Updated
- 2021/12/16
- Product number
- CS-0035381
- Product name
- Pz-1
- Purity
- >99.0%
- Packaging
- 25mg
- Price
- $790
- Updated
- 2021/12/16
- Product number
- CS-0035381
- Product name
- Pz-1
- Purity
- >99.0%
- Packaging
- 5mg
- Price
- $220
- Updated
- 2021/12/16
PZ-1 Chemical Properties,Usage,Production
Biological Activity
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 th at 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 Preparation Products And Raw materials
Raw materials
Preparation Products
PZ-1 Suppliers
- Tel
- --
- Fax
- --
- sialjp@sial.com
- Country
- Japan
- ProdList
- 5753
- Advantage
- 58