Description
Pz-1 is a potent RET and VEGFR2 inhibitor with IC50s of less than 1 nM for both wild type kinases.
Product information
CAS Number: 1800505-64-9
Molecular Weight: 454.52
Formula: C26H26N6O2
Chemical Name: N-(5-tert-butyl-1,2-oxazol-3-yl)-2-{4-[5-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-1-yl]phenyl}acetamide
Smiles: CN1C=C(C=N1)C1C=C2N=CN(C2=CC=1)C1C=CC(CC(=O)NC2C=C(ON=2)C(C)(C)C)=CC=1
InChiKey: NJLMIILZNLZZFW-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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 (RETV804M and RETV804L).
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.
Products are for research use only. Not for human use.
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