Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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Other Sizes |
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Purity: ≥98%
PF-4618433 is a novel, potent and selective inhibitor of proline-rich tyrosine kinase 2 (PYK2) and focal adhesion kinase (FAK), showing improved PYK2 potency, reduced p38 activity, and superior overall selectivity relative to the prototype BIRB796.
Targets |
PYK2 (IC50 = 637 nM)
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ln Vitro |
In hMSC cultures, PF-4618433 (0.1-1.0 μM; 7 days) stimulates osteogenesis. Alkaline phosphatase (ALP) activity and mineralization are increased by PF-4618433 in a drug-dependent way [1]. At dosages of 0.1 and 0.3 μM, PF-4618433 (0.0125-0.3 μM; 14 or 21 days) improves calcium deposition [2]. μM; 24 hours) increases the proliferation of osteoblasts [2].
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Cell Assay |
Cell Proliferation Assay[2] Cell
Cell Types: mouse bone marrow-derived mesenchymal stem cells (BMSC) Tested Concentrations: 0.1, 0.3 μM Incubation Duration: 24 hrs (hours) Experimental Results: Compared with the untreated group or control group, cell proliferation activity increased Dramatically . |
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. |
Molecular Formula |
C24H27N7O2
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Molecular Weight |
445.52
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Exact Mass |
445.2226
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Elemental Analysis |
C, 64.70; H, 6.11; N, 22.01; O, 7.18
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CAS # |
1166393-85-6
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Related CAS # |
1166393-85-6
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Appearance |
Solid powder
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SMILES |
CC1=CC=C(C=C1)N2C(=CC(=N2)C(C)(C)C)NC(=O)NC3=NNC(=C3)COC4=CN=CC=C4
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InChi Key |
NJARPUHZDSAXPL-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C24H27N7O2/c1-16-7-9-18(10-8-16)31-22(13-20(30-31)24(2,3)4)27-23(32)26-21-12-17(28-29-21)15-33-19-6-5-11-25-14-19/h5-14H,15H2,1-4H3,(H3,26,27,28,29,32)
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Chemical Name |
1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[5-(pyridin-3-yloxymethyl)-1H-pyrazol-3-yl]urea
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Synonyms |
PF-4618433; PF4618433; PF 4618433
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~100 mg/mL (~224.5 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.61 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2446 mL | 11.2228 mL | 22.4457 mL | |
5 mM | 0.4489 mL | 2.2446 mL | 4.4891 mL | |
10 mM | 0.2245 mL | 1.1223 mL | 2.2446 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Three-dimensional structure of PYK2:PF-4618433 complex from human. J Biol Chem . 2009 May 8;284(19):13193-201. td> |
PF-4618433 promotes osteogenesis of hMSC cultures. J Biol Chem . 2009 May 8;284(19):13193-201. td> |