Home Protein Tyrosine Kinase PDGFR inhibitor - VEGFR inhibitor - FLT3 inhibitor - c-Kit inhibitor AZD2932 For research use only.

AZD2932

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 Chemical Structure

AZD2932 Chemical Structure

CAS No. 883986-34-3

Purity & Quality Control

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

AZD2932 Related Products

Signaling Pathway

PDGFR Signaling Pathways

PDGFR Signaling Pathway

Biological Activity

Description 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.
Targets
PDGFRβ [1] Flt3 [1] VEGFR-2 [1] c-Kit [1]
4 nM 7 nM 8 nM 9 nM
In vitro
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). AZD2932 inhibits both PDGFRα and PDGFRβ phosphorylation with a correlation close to 1:1. AZD2932 does not inhibit the various cytochrome P450 isoforms with the worst IC50 being against 2C9 (8.0 μM). AZD2932 has no activity against hERG (IC50, 137 μM).[1]
In Vivo
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.). AZD2932 (3–50 mg/kg, p.o.) causes 60–80% inhibition of both p-VEGFR-2 and p-PDGFRβ. Single bolus oral doses of AZD2932 results in dose-related inhibition of PDGFRa phosphorylation 6 h after dosing.[1]

Chemical Information & Solubility

Molecular Weight 447.49 Formula

C24H25N5O4
CAS No. 883986-34-3 SDF Download AZD2932 SDF
Smiles CC(C)N1C=C(C=N1)NC(=O)CC2=CC=C(C=C2)OC3=NC=NC4=CC(=C(C=C43)OC)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 89 mg/mL ( (198.88 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : 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. )

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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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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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