1166393-85-6

1166393-85-6 structure

Name: PF-4618433
Chemical Name: 1-(3-(tert-butyl)-1-(p-tolyl)-1H-pyrazol-5-yl)-3-(5-((pyridin-3-yloxy)methyl)-1H-pyrazol-3-yl)urea
CAS Number: 1166393-85-6
Molecular Formula: C₂₄H₂₇N₇O₂
Molecular Weight: 445.517
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Pyk2
Create Date: 2016-07-15 22:31:24
Modify Date: 2024-01-10 17:56:00
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].

Name	1-(3-(tert-butyl)-1-(p-tolyl)-1H-pyrazol-5-yl)-3-(5-((pyridin-3-yloxy)methyl)-1H-pyrazol-3-yl)urea
Synonyms	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

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.