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PF-4618433

Names

[ CAS No. ]:
1166393-85-6

[ Name ]:
PF-4618433

[Synonym ]:
1-(3-(tert-butyl)-1-(p-tolyl)-1H-pyrazol-5-yl)-3-(3-((pyridin-3-yloxy)methyl)-1H-pyrazol-5-yl)urea
1-[1-(4-Methylphenyl)-3-(2-methyl-2-propanyl)-1H-pyrazol-5-yl]-3-{3-[(3-pyridinyloxy)methyl]-1H-pyrazol-5-yl}urea
Urea, N-[3-(1,1-dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl]-N'-[3-[(3-pyridinyloxy)methyl]-1H-pyrazol-5-yl]-
PF4618433

Biological Activity

[Description]:

PF-4618433 is a potent and selective PYK2 inhibitor, with an IC50 of 637 nM. PF-4618433 may be suitable for the research of osteoporosis, craniofacial and appendicular skeletal defects and for targeted bone regeneration[1][2].

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Pyk2
Research Areas >> Metabolic Disease

[Target]

IC50: 637 nM (PYK2)[1]


[In Vitro]

PF-4618433 (0.1-1.0 μM; 7 days) promotes osteogenesis of hMSC cultures. PF-4618433 increases in both alkaline phosphatase (ALP) activity and mineralization in a dependent manner[1]. PF-4618433 (0.1-0.3 μM; 24 hours) enhances osteoblast proliferation[2]. PF-4618433 (0.0125-0.3 μM; 14 or 21 days) enhances calcium deposition at the concentrations of 0.1 and 0.3 μM[2]. Cell Proliferation Assay[2] Cell Line: Murine bone marrow-derived mesenchymal stem cells (BMSC) Concentration: 0.1, 0.3 μM Incubation Time: 24 hours Result: Increased cell proliferation activity significantly when compared to the untreated or control group.

[References]

[1]. Seungil H, et, al. Structural Characterization of Proline-Rich Tyrosine Kinase 2 (PYK2) Reveals a Unique (DFG-out) Conformation and Enables Inhibitor Design. J Biol Chem. 2009 May 8; 284(19): 13193-201.

[2]. Sumana P, et, al. A Pyk2 Inhibitor Incorporated Into a PEGDA-gelatin Hydrogel Promotes Osteoblast Activity and Mineral Deposition. Biomed Mater. 2019 Feb 27; 14(2): 025015.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
587.6±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C24H27N7O2

[ Molecular Weight ]:
445.517

[ Flash Point ]:
309.2±30.1 °C

[ Exact Mass ]:
445.222626

[ PSA ]:
109.75000

[ LogP ]:
4.86

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.649

Related Compounds