Pz-1 - 10mM in DMSO , CAS No.1800505-64-9

CAS: 1800505-64-9 Cat. No.: P655307 Molecular Weight: 454.52 PubChem CID: 102004343

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Pz-1 is a potent RET and VEGFR2 inhibitor with IC 50 s of less than 1 nM for both wild type kinases.

In Vitro

Pz-1 is a Type-II tyrosine kinase inhibitor, able to bind the DFG-out conformation of the kinase. In cell-based assays, 1.0 nM of Pz-1 strongly inhibits tyrosine phosphorylation of VEGFR2 and clinically relevant RET mutants, including those refractory to vandetanib and cabozantinib (RET V804M and RET V804L ). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Pz-1 is shown active on VEGFR2, which can block blood supply required for RET-stimulated growth. At 1.0 mg/kg/day per os, Pz-1 abrogates formation of tumors induced by RET-mutant fibroblasts and blocks phosphorylation of both RET and VEGFR2 in tumor tissue. Pz-1 features no detectable toxicity up to 100.0 mg/kg, which indicates a large therapeutic window . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:IC50: < 1 nM (RET and VEGFR2)

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Pz-1 is a potent RET and VEGFR2 inhibitor with IC 50 s of less than 1 nM for both wild type kinases.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Names and Identifiers

• Isomeric SMILES: CC(C)(C)C1=CC(=NO1)NC(=O)CC2=CC=C(C=C2)N3C=NC4=C3C=CC(=C4)C5=CN(N=C5)C
• PubChem CID: 102004343
• Molecular Weight: 454.52