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Details

Stereochemistry ACHIRAL
Molecular Formula C26H27N3O5
Molecular Weight 461.5107
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PF-337210

SMILES

Cc1c(c2ccc(cc2o1)Oc3ccnc4cc(ccc43)OCCN5CCOCC5)C(=NC)O

InChI

InChIKey=LGXVKMDGSIWEHL-UHFFFAOYSA-N
InChI=1S/C26H27N3O5/c1-17-25(26(30)27-2)21-6-4-19(16-24(21)33-17)34-23-7-8-28-22-15-18(3-5-20(22)23)32-14-11-29-9-12-31-13-10-29/h3-8,15-16H,9-14H2,1-2H3,(H,27,30)

HIDE SMILES / InChI

Molecular Formula C26H27N3O5
Molecular Weight 461.5107
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Approval Year

Substance Class Chemical
Created
by admin
on Sat Jun 26 07:20:58 UTC 2021
Edited
by admin
on Sat Jun 26 07:20:58 UTC 2021
Record UNII
3K3KYC9LES
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PF-337210
Common Name English
N,2-DIMETHYL-6-(7-(2-MORPHOLIN-4-YLETHOXY)QUINOLIN-4-YL)OXY-1-BENZOFURAN-3-CARBOXAMIDE
Systematic Name English
3-BENZOFURANCARBOXAMIDE, N,2-DIMETHYL-6-((7-(2-(4-MORPHOLINYL)ETHOXY)-4-QUINOLINYL)OXY)-
Systematic Name English
PF-00337210
Common Name English
Code System Code Type Description
PUBCHEM
11236560
Created by admin on Sat Jun 26 07:20:59 UTC 2021 , Edited by admin on Sat Jun 26 07:20:59 UTC 2021
PRIMARY
MANUFACTURER PRODUCT INFORMATION
PF-337210
Created by admin on Sat Jun 26 07:20:59 UTC 2021 , Edited by admin on Sat Jun 26 07:20:59 UTC 2021
PRIMARY PF-00337210 is an orally available ATP-competitive inhibitor of the vascular endothelial growth factor receptor type 2 (VEGFR2), with potential anti-angiogenesis and antineoplastic activities. Upon administration, the VEGFR2 tyrosine kinase inhibitor PF-00337210 selectively binds to VEGFR2 and prevents its phosphorylation which may result in an inhibition of migration, proliferation and survival of endothelial cells, microvessel formation, the inhibition of tumor cell proliferation, and may eventually cause tumor cell death. VEGFR2, a receptor tyrosine kinase, is frequently overexpressed by a variety of tumor types.
FDA UNII
3K3KYC9LES
Created by admin on Sat Jun 26 07:20:59 UTC 2021 , Edited by admin on Sat Jun 26 07:20:59 UTC 2021
PRIMARY
CAS
854514-88-8
Created by admin on Sat Jun 26 07:20:59 UTC 2021 , Edited by admin on Sat Jun 26 07:20:59 UTC 2021
PRIMARY
ChEMBL
CHEMBL3545136
Created by admin on Sat Jun 26 07:20:59 UTC 2021 , Edited by admin on Sat Jun 26 07:20:59 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
Related Record Type Details
ACTIVE MOIETY
PF-00337210 is a potent, selective, and orally bioavailable small molecule inhibitor of VEGFRs. It is an ATP-competitive compound that is selective for VEGFR-2 when biochemically profiled against >100 diverse tyrosine and serine-threonine kinases. PF-00337210 preferentially binds to the unactivated kinase (Ki=0.7 nM) relative to the fully phosphorylated form (Ki= 8.8 nM). Crystallographic evidence suggests that its selectivity is likely a result of its ability to bind to a DFG-out conformation of VEGFR-2. In the cell, PF-00337210 inhibits the auto-phosphorylation of human and murine VEGFR-2 with IC50s of 0.87 +/- 0.11 nM and 0.83 +/- 0.29 nM, respectively.