[CAS NO. 1166393-85-6] PF-4618433
PRODUCTS SPECIFICATIONS [1166393-85-6]
DESCRIPTION [1166393-85-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 445.52 |
| Molecular Formula | C24H27N7O2 |
| SMILES | O=C(NC1=CC(COC2=CC=CN=C2)=NN1)NC3=CC(C(C)(C)C)=NN3C4=CC=C(C)C=C4 |
Summary
IC50 & 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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 125 mg/mL ( 280.57 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
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.