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PDGFR&FGFR

AZD2932 (883986-34-8)

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.

Not Intended for Therapeutic Use. For research use only.

CAS: 883986-34-8 Category

AZD2932 (883986-34-8) Description:

AZD-2932 is a high affinity inhibitor of VEFGR-2 and PDGFR. AZD-2932 has a balanced ~ 1:1 ratio of activity vs both VEGFR-2 and PDGFRβ and shows IC50 values of 8 and 4 nM against the two enzymes, respectively. It is also active on c-Kit and FLT3 with good selectivity on a panel of kinases. The pharmacokinetic behavior and the preclinical antitumor activity in nude mice bearing C6 rat glial tumors indicate that 31 has the potential to become an antiangiogenic agent in the clinic.

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 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.

AZD2932 (883986-34-8) Specifications:

Product Name AZD2932
Synonym AZD2932; AZD 2932; AZD-2932
Chemical Name 2-(4-((6,7-dimethoxyquinazolin-4-yl)oxy)phenyl)-N-(1-isopropyl-1H-pyrazol-4-yl)acetamide
Purity ≥98% (HPLC)
CAS Number 883986-34-8
Molecular Formula C24H25N5O4
Molecular Weight 447.495 g/mol
Monoisotopic Mass 447.191 g/mol
MDL number N/A
InChIKey TWYCZJMOEMMCGC-UHFFFAOYSA-N
InChi Code InChI=1S/C24H25N5O4/c1-15(2)29-13-17(12-27-29)28-23(30)9-16-5-7-18(8-6-16)33-24-19-10-21(31-3)22(32-4)11-20(19)25-14-26-24/h5-8,10-15H,9H2,1-4H3,(H,28,30)
SMILES O=C(NC1=CN(C(C)C)N=C1)CC2=CC=C(OC3=C4C=C(OC)C(OC)=CC4=NC=N3)C=C2
Form Powder
Color N/A
Solubility  DMSO 89 mg/mL (198.89 mM)

Water Insoluble

Alcohol 5 mg/mL (11.17 mM)

Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application affinity inhibitor of VEFGR-2 and PDGFR

 


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RIDADR NONH for all modes of transport

References:

[1]. Plé PA, Jung F, Ashton S, Hennequin L, Laine R, Morgentin R, Pasquet G, Taylor S. 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. doi: 10.1016/j.bmcl.2011.11.019. Epub 2011 Nov 12. PubMed PMID: 22153662.

1 review for AZD2932 (883986-34-8)

  1. Cofttek

    Never had such good experience before,The AZD2932 (883986-34-8) is high purity,also customer service is pretty nice !gotta try!!

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