Pz-1

Modify Date: 2024-01-16 18:20:10

Pz-1 structure	Common Name	Pz-1
	CAS Number	1800505-64-9	Molecular Weight	454.52
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₆H₂₆N₆O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Pz-1

Pz-1 is a potent RET and VEGFR2 inhibitor with IC50s of less than 1 nM for both wild type kinases.

Name	Pz-1

Description	Pz-1 is a potent RET and VEGFR2 inhibitor with IC50s of less than 1 nM for both wild type kinases.
Related Catalog	Research Areas >> Cancer Research Areas >> Cardiovascular Disease
Target	IC50: < 1 nM (RET and VEGFR2)[1]
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)[1].
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[1].
Animal Admin	Mice[1] In order to address in vivo RET-driven effects, Pz-1 is tested on tumors induced by oncogenic RET compared to a constitutively-active control Ras oncogene. Immunodeficient (nu/nu) mice are then injected with NIH3T3 RETC634Y or NIH3T3 HRasG12V cells and, before tumors have appeared, treated PO with Pz-1 (1.0, 3.0 or 10.0 mg/kg/day) or left untreated. Then the tumor effects are measured[1]
References	[1]. Frett B, et al. Fragment-Based Discovery of a Dual pan-RET/VEGFR2 Kinase Inhibitor Optimized for Single-Agent Polypharmacology. Angew Chem Int Ed Engl. 2015 Jul 20;54(30):8717-21.

Molecular Formula	C₂₆H₂₆N₆O₂
Molecular Weight	454.52

Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Pz-1
Price: Negotiable
Purity: 99.95%
Delivery: 10 Day
Contact: Huang
Email: sales@echemcloud.com

ShangHai DC Chemicals Co.,Ltd
China
Product Name: Pz-1
Price: ￥Inquiry/1g
Purity: 98.9%
Delivery: 1 Day
Contact: Tony Lai
Email: order@dcchemicals.com

DC Chemicals Limited
China
Product Name: Pz-1
Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
Purity: 98.0%
Delivery: 3 Day
Contact: Tony Cao
Email: sales@dcchemicals.com

Get all suppliers and price by the below link:

Price: $80/5mg

Reference only. check more Pz-1 price