1. Protein Tyrosine Kinase/RTK
  2. RET
    VEGFR
  3. Pz-1

Pz-1 

Cat. No.: HY-U00437 Purity: >99.0%
Handling Instructions

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

For research use only. We do not sell to patients.

Pz-1 Chemical Structure

Pz-1 Chemical Structure

CAS No. : 1800505-64-9

Size Price Stock
10 mM * 1 mL in DMSO USD 242 Ask For Quote & Lead Time
5 mg USD 220 Ask For Quote & Lead Time
10 mg USD 390 Ask For Quote & Lead Time
25 mg USD 790 Ask For Quote & Lead Time

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Description

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

IC50 & 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].

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

454.52

Formula

C₂₆H₂₆N₆O₂

CAS No.

1800505-64-9

SMILES

O=C(NC1=NOC(C(C)(C)C)=C1)CC2=CC=C(N3C4=CC=C(C5=CN(C)N=C5)C=C4N=C3)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References
Animal Administration
[1]

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]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: >99.0%

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Keywords:

Pz-1Pz1Pz 1RETVEGFRVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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