JK-P3 | CAS# 942655-44-9 | novel inhibitor of VEGFR-2

MedKoo Cat#: 581057 | Name: JK-P3

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Description:

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

JK-P3 is novel inhibitor of VEGFR-2. JK-P3 is a pyrazole-based inhibitor of VEGFR-2 (IC50 = 7.8 μM). JK-P3 inhibits FGFR 1/3 kinase activity in vitro, but has no effect on FGFR signaling in cell-based assays. The compound blocks wound healing and tube formation in HUVEC without effecting endothelial cell proliferation.

Chemical Structure

JK-P3

CAS#942655-44-9

Theoretical Analysis

MedKoo Cat#: 581057

Name: JK-P3

CAS#: 942655-44-9

Chemical Formula: C18H17N3O3

Exact Mass: 323.1270

Molecular Weight: 323.35

Elemental Analysis: C, 66.86; H, 5.30; N, 13.00; O, 14.84

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 350.00	2 Weeks
25mg	USD 700.00	2 Weeks

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Synonym

JK-P3, 3,4-Dimethoxy-N-(5-phenyl-1H-pyrazol-3-yl)-benzamide

IUPAC/Chemical Name

3,4-Dimethoxy-N-(5-phenyl-1H-pyrazol-3-yl)-benzamide

InChi Key

QAZJUVDICQNITG-UHFFFAOYSA-N

InChi Code

InChI=1S/C18H17N3O3/c1-23-15-9-8-13(10-16(15)24-2)18(22)19-17-11-14(20-21-17)12-6-4-3-5-7-12/h3-11H,1-2H3,(H2,19,20,21,22)

SMILES Code

O=C(NC1=NNC(C2=CC=CC=C2)=C1)C3=CC=C(OC)C(OC)=C3

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

Shelf Life

>2 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

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Product Data

Product Data

Instruction

View handling instruction

Biological target:

JK-P3 is a potent and pan VEGFR2 inhibitor, with IC50s of 7.83 μM, 27 μM and 5.18 μM for VEGFR2, FGFR1 and FGFR3, respectively.

In vitro activity:

JK-P3 and JK-P5 were predicted to bind the VEGFR2 kinase domain with high affinity, and both compounds showed pronounced inhibition of endogenous VEGFR2 kinase activity in primary human endothelial cells. Only JK-P3 inhibited VEGF-A-stimulated VEGFR2 activation and intracellular signalling. Interestingly, JK-P3 inhibited endothelial monolayer wound closure and angiogenesis but not endothelial cell proliferation. Reference: Br J Pharmacol. 2012 May;166(2):737-48. https://pubmed.ncbi.nlm.nih.gov/22141913/

In vivo activity:

TBD

Preparing Stock Solutions

The following data is based on the product molecular weight 323.35 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.

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:

1. Kankanala J, Latham AM, Johnson AP, Homer-Vanniasinkam S, Fishwick CW, Ponnambalam S. A combinatorial in silico and cellular approach to identify a new class of compounds that target VEGFR2 receptor tyrosine kinase activity and angiogenesis. Br J Pharmacol. 2012 May;166(2):737-48. doi: 10.1111/j.1476-5381.2011.01801.x. PMID: 22141913; PMCID: PMC3417501.

In vitro protocol:

In vivo protocol:

TBD

1: Kankanala J, Latham AM, Johnson AP, Homer-Vanniasinkam S, Fishwick CW, Ponnambalam S. A combinatorial in silico and cellular approach to identify a new class of compounds that target VEGFR2 receptor tyrosine kinase activity and angiogenesis. Br J Pharmacol. 2012 May;166(2):737-48. doi: 10.1111/j.1476-5381.2011.01801.x. PubMed PMID: 22141913; PubMed Central PMCID: PMC3417501.