Home Protein Tyrosine Kinase VEGFR inhibitor - c-RET inhibitor WHI-P180 For research use only.

WHI-P180

WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET (c-RET) and kinase insert domain receptor (KDR), respectively.

WHI-P180 Chemical Structure

WHI-P180 Chemical Structure

CAS No. 211555-08-7

Purity & Quality Control

WHI-P180 Related Products

Signaling Pathway

VEGFR Signaling Pathways

VEGFR Signaling Pathway

Biological Activity

Description WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET (c-RET) and kinase insert domain receptor (KDR), respectively.
Targets
RET [1]
(Cell-free assay)		 KDR [1]
(Cell-free assay)
4.5 nM 66 nM
In Vivo
In vivo

The elimination half-life of WHI-P180 in CD-1 mice (BALB/ c mice) following i.v., i.p., or p.o. administration is less than 10 min. Systemic clearance of WHI-P180 is 6742 mL/h/kg in CD-1 mice and 8188 mL/h/kg in BALB/c mice. Notably, WHI-P180, when administered in two consecutive nontoxic i.p. bolus doses of 25 mg/kg, inhibited IgE/antigen-induced vascular hyperpermeability in a well-characterized murine model of passive cutaneous anaphylaxis[2].

Chemical Information & Solubility

Molecular Weight 297.31 Formula

C16H15N3O3
CAS No. 211555-08-7 SDF --
Smiles COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)O)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 59 mg/mL ( (198.44 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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