[CAS NO. 883986-34-3]  AZD2932

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PRODUCTS SPECIFICATIONS [883986-34-3]

Store
Catalog
SLK-S7003
Brand
Selleck
CAS
883986-34-3

DESCRIPTION [883986-34-3]

Overview

MDL-
Molecular Weight447.49
Molecular FormulaC24H25N5O4
SMILES-

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.2347 mL11.1734 mL22.3469 mL
5 mM0.4469 mL2.2347 mL4.4694 mL
10 mM0.2235 mL1.1173 mL2.2347 mL
50 mM0.0447 mL0.2235 mL0.4469 mL

Description

AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with of 8 nM, 4 nM, 7 nM, and 9 nM for , , , and , respectively.

Targets

PDGFRβ [1]Flt3 [1]VEGFR-2 [1]c-Kit [1]
4 nM7 nM8 nM9 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). 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).

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.