AZD2932

Cat. No.: HY-18179 Purity: 99.04%: FAQs
Data Sheet SDS COA Handling Instructions

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AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC₅₀s of 8, 4, 7 and 9 nM in cell assay, respectively.

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

AZD2932 Chemical Structure

CAS No. : 883986-34-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 77	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 77	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 320	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 510	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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PDGFR PDGFRβ PDGFRα

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC₅₀s of 8, 4, 7 and 9 nM in cell assay, respectively.

IC₅₀ & Target^[1]

VEGFR2

8 nM (IC₅₀)

PDGFRβ

4 nM (IC₅₀)

FLT3

7 nM (IC₅₀)

c-Kit

9 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	> 10 μM Compound: 15; AZD2932	Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay	[PMID: 30204441]
BaF3	GI₅₀	> 10000 nM Compound: 1; AZD2932	Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 30565931]
BaF3	GI₅₀	2 nM Compound: 1; AZD2932	Antiproliferative activity against mouse BaF3 cells transfected with FLT3 ITD mutant assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells transfected with FLT3 ITD mutant assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 30565931]
BaF3	GI₅₀	3.1 nM Compound: 1; AZD2932	Antiproliferative activity against mouse BaF3 cells transfected with TEL-fused FLT3 assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells transfected with TEL-fused FLT3 assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 30565931]
BaF3	GI₅₀	45 nM Compound: 1; AZD2932	Antiproliferative activity against mouse BaF3 cells transfected with TEL-fused cKIT assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells transfected with TEL-fused cKIT assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 30565931]

In Vitro

AZD2932 has a potent and balanced profile against PDGFβ, VEGFR-2, Flt-3 and c-Kit. It 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].

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

In Vivo

Twice daily oral dosing (b.i.d.) of AZD2932 10 h apart results in significant tumor growth inhibition of 64% for both 50 and 12.5 mg/kg doses on the day the control animals are terminated. Xenografts bearing non PDGFβ expressing tumor cells are also sensitive to AZD2932 treatment: growth of Calu-6 tumor is inhibited by 81% and 72% at 50 and 12.5 mg/kg b.i.d. and and LoVo tumors by 67% at 50 mg/kg b.i.d. This is due AZD2932 potent activity against VEGFR2 as well as a potential effect on pericytes and tumor-associated fibroblasts due to PDGFR a and b inhibition. AZD2932 at 3–50 mg/kg b.i.d. 10 h apart gives 60–80% inhibition of both p-VEGFR2 and p-PDGFβ in a 1:1 ratio^[1].

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

Molecular Weight

447.49

Formula

C₂₄H₂₅N₅O₄

CAS No.

883986-34-3

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CN(C(C)C)N=C1)CC2=CC=C(OC3=C4C=C(OC)C(OC)=CC4=NC=N3)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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 10 mg/mL (22.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2347 mL	11.1734 mL	22.3469 mL
5 mM	0.4469 mL	2.2347 mL	4.4694 mL
10 mM	0.2235 mL	1.1173 mL	2.2347 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.23 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1 mg/mL (2.23 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1 mg/mL (2.23 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.04%

Select Batch:

Data Sheet (277 KB) SDS (392 KB)

COA (251 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[1]. Plé PA, et al. Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases. Bioorg Med Chem Lett. 2012 Jan 1;22(1):262-6. [Content Brief]

Animal Administration
^[1]

Mice: To confirm that AZD2932 has similar potency against both PDGFβ and VEGFR-2 phosphorylation, the female nude mice bearing C6 tumors are dosed iv with VEGF-A and PDGF_BB 5 min prior to cull and 6 h post last dose of AZD2932 and the lungs excised immediately after. Lung lysates are analyzed by western blot for total and phosphorylated VEGFR-2 and PDGFβ^[1].

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

References

[1]. Plé PA, et al. Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases. Bioorg Med Chem Lett. 2012 Jan 1;22(1):262-6. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2347 mL	11.1734 mL	22.3469 mL	55.8672 mL
	5 mM	0.4469 mL	2.2347 mL	4.4694 mL	11.1734 mL
	10 mM	0.2235 mL	1.1173 mL	2.2347 mL	5.5867 mL
	15 mM	0.1490 mL	0.7449 mL	1.4898 mL	3.7245 mL
	20 mM	0.1117 mL	0.5587 mL	1.1173 mL	2.7934 mL

AZD2932 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZD2932883986-34-3AZD 2932AZD-2932PDGFRVEGFRFLT3c-KitPlatelet-derived growth factor receptorVascular endothelial growth factor receptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3SCFRCD117Inhibitorinhibitorinhibit

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AZD2932

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Complete Stock Solution Preparation Table

AZD2932 Related Classifications

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