Home Protein Tyrosine Kinase PDGFR inhibitor AZD2932

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AZD2932 PDGFR inhibitor

Cat.No.S7003

AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.
AZD2932 PDGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 447.49

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Quality Control

Batch: S700301 DMSO]89 mg/mL]false]Ethanol]5 mg/mL]false]Water]Insoluble]false Purity: 99.59%
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99.59

Solubility

In vitro
Batch:

DMSO : 89 mg/mL (198.88 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

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

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Chemical Information, Storage & Stability

Molecular Weight 447.49 Formula

C24H25N5O4

 Storage (From the date of receipt)
CAS No. 883986-34-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC(C)N1C=C(C=N1)NC(=O)CC2=CC=C(C=C2)OC3=NC=NC4=CC(=C(C=C43)OC)OC

Mechanism of Action

Targets/IC50/Ki
PDGFRβ
4 nM
Flt3
7 nM
VEGFR-2
8 nM
c-Kit
9 nM
In vitro
AZD2932 effectively inhibits the activities of VEGFR-2 (IC50, 8 nM), PDGFRβ (IC50,4 nM), Flt-3 (IC50, 7 nM), and c-Kit (IC50, 9 nM). This compound inhibits both PDGFRα and PDGFRβ phosphorylation with a correlation close to 1:1. It does not inhibit the various cytochrome P450 isoforms with the worst IC50 being against 2C9 (8.0 μM). It has no activity against hERG (IC50, 137 μM).
In vivo
In C6 rat glial tumor model, AZD2932 (p.o., b.i.d.) results in significant TGI of 64% for both 50 and 12.5 mg/kg doses. Growth of Calu-6 tumor is inhibited by 81% and 72% at 50 and 12.5 mg/kg b.i.d. (p.o.) and LoVo tumors by 67% at 50 mg/kg b.i.d (p.o.). This compound (3–50 mg/kg, p.o.) causes 60–80% inhibition of both p-VEGFR-2 and p-PDGFRβ. Single bolus oral doses of this chemical results in dose-related inhibition of PDGFRa phosphorylation 6 h after dosing.
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