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.

Chemical Structure

img
PF-00337210
CAS# 854514-88-8
Instruction

Theoretical Analysis

MedKoo Cat#: 205916
Name: PF-00337210
CAS#: 854514-88-8
Chemical Formula: C26H27N3O5
Exact Mass: 461.20
Molecular Weight: 461.510
Elemental Analysis: C, 67.66; H, 5.90; N, 9.10; O, 17.33

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

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

InChi Key: LGXVKMDGSIWEHL-UHFFFAOYSA-N

InChi Code: 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)

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

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).

HS Tariff Code: 2934.99.9001

More Info: 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).          

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 461.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

 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.