Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C26H27N3O5 |
| Molecular Weight | 461.5097 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CNC(=O)C1=C(C)OC2=CC(OC3=CC=NC4=CC(OCCN5CCOCC5)=CC=C34)=CC=C12
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)
| Molecular Formula | C26H27N3O5 |
| Molecular Weight | 461.5097 |
| 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
Edited
Sat Dec 16 10:58:24 GMT 2023
by
admin
on
Sat Dec 16 10:58:24 GMT 2023
|
| Record UNII |
3K3KYC9LES
|
| Record Status |
Validated (UNII)
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| Record Version |
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-
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Common Name | English | ||
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Common Name | English |
| Code System | Code | Type | Description | ||
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11236560
Created by
admin on Sat Dec 16 10:58:24 GMT 2023 , Edited by admin on Sat Dec 16 10:58:24 GMT 2023
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PF-337210
Created by
admin on Sat Dec 16 10:58:24 GMT 2023 , Edited by admin on Sat Dec 16 10:58:24 GMT 2023
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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. | ||
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C97950
Created by
admin on Sat Dec 16 10:58:24 GMT 2023 , Edited by admin on Sat Dec 16 10:58:24 GMT 2023
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3K3KYC9LES
Created by
admin on Sat Dec 16 10:58:24 GMT 2023 , Edited by admin on Sat Dec 16 10:58:24 GMT 2023
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854514-88-8
Created by
admin on Sat Dec 16 10:58:24 GMT 2023 , Edited by admin on Sat Dec 16 10:58:24 GMT 2023
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300000042567
Created by
admin on Sat Dec 16 10:58:24 GMT 2023 , Edited by admin on Sat Dec 16 10:58:24 GMT 2023
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CHEMBL3545136
Created by
admin on Sat Dec 16 10:58:24 GMT 2023 , Edited by admin on Sat Dec 16 10:58:24 GMT 2023
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PRIMARY |
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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.
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