1. Protein Tyrosine Kinase/RTK
  2. PDGFR
    VEGFR
    FLT3
    c-Kit
  3. AZD2932

AZD2932 

Cat. No.: HY-18179 Purity: 98.12%
Handling Instructions

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

AZD2932 Chemical Structure

CAS No. : 883986-34-3

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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)

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].

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].

Molecular Weight

447.49

Formula

C₂₄H₂₅N₅O₄

CAS No.

883986-34-3

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 41 mg/mL (91.62 mM)

*"≥" means soluble, but saturation unknown.

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
*Please refer to the solubility information to select the appropriate solvent.
References
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 PDGFBB 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

Purity: 98.12%

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AZD2932
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HY-18179
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