Home Protein Tyrosine Kinase c-Kit inhibitor - PDGFR inhibitor AZD3229 For research use only.

AZD3229

AZD3229 is a potent, pan-Kit (c-Kit) mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant Kit (c-Kit) driven Ba/F3 cell lines (GI50=1-50 nM), with good margin to KDR-driven effects. It also inhibits PDGFR mutants (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V).

AZD3229 Chemical Structure

AZD3229 Chemical Structure

CAS No. 2248003-60-1

Purity & Quality Control

AZD3229 Related Products

Signaling Pathway

c-Kit Signaling Pathways

c-Kit Signaling Pathway

Biological Activity

Description AZD3229 is a potent, pan-Kit (c-Kit) mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant Kit (c-Kit) driven Ba/F3 cell lines (GI50=1-50 nM), with good margin to KDR-driven effects. It also inhibits PDGFR mutants (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V).
Targets
Kit [1] PDGFRα [1] PDGFRβ [1]
In Vivo
In vivo

In preclinical species, bioavailability is high and clearance low across all of mouse, rat, and dog. Volume of distribution is low consistent with the neutral structure[1]. In in vivo models using Ba/F3 cell lines, AZD3229 at a dose of 20 mg/kg b.i.d induces tumor volume regression more effectively[2].

Chemical Information & Solubility

Molecular Weight 479.51 Formula

C24H26FN7O3
CAS No. 2248003-60-1 SDF --
Smiles CC(C)C1=CN(N=N1)CC(=O)NC2=CC=C(C=C2)NC3=NC=NC4=C3C(=CC(=C4)OCCOC)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 96 mg/mL ( (200.2 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : ˂1 mg/mL

Ethanol : ˂1 mg/mL


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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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