PF-00337210

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 205916

CAS#: 854514-88-8

Description: 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.


Price and Availability

Size
Price

Size
Price

Size
Price

PF-00337210 is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

img

Theoretical Analysis

MedKoo Cat#: 205916
Name: PF-00337210
CAS#: 854514-88-8
Chemical Formula: C26H27N3O5
Exact Mass: 461.19507
Molecular Weight: 461.51
Elemental Analysis: C, 67.66; H, 5.90; N, 9.10; O, 17.33


Synonym: PF00337210; PF 00337210; PF-00337210; P337210; PF-337210; PF337210.

IUPAC/Chemical Name: N,2-dimethyl-6-((7-(2-morpholinoethoxy)quinolin-4-yl)oxy)benzofuran-3-carboxamide

SMILES Code: O=C(C1=C(C)OC2=CC(OC3=CC=NC4=CC(OCCN5CCOCC5)=CC=C34)=CC=C12)NC


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not soluble in water.

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

PF-00337210 is a highly potent and selective ATP-competitive inhibitor of VEGFR2 TK with a cellular IC50 of 0.8 nM. In vivo, it inhibits tumor angiogenesis and human xenograft growth. Modulation of blood pressure (BP) and vascular permeability (volume transfer constant: Ktrans) appear to be suitable markers of efficacy for VEGF/VEGFR inhibitors.  PF-00337210 is well tolerated at 6 mg BID, with profound VEGFR inhibition effects (as measured by elevated BP and a significant decrease in tumor vascular parameters by DCE-MRI). (source: http://www.asco.org/ASCOv2/Meetings/Abstracts?&vmview=abst_detail_view&confID=74&abstractID=50129).
   
 
 
 


References

 1: Marra MT, Khamphavong P, Wisniecki P, Gukasyan HJ, Sueda K. Solution formulation development of a VEGF inhibitor for intravitreal injection. AAPS PharmSciTech. 2011 Mar;12(1):362-71. Epub 2011 Feb 11. PubMed PMID: 21312012; PubMed Central PMCID: PMC3066352.