PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively. Treatment with PF-562271 impaires cell viability in all cell lines, with an average IC50 of 2.4 μM after 3 days of treatment. TC32 and A673 are the 2 most sensitive cell lines, with IC50 concentrations of 2.1 and 1.7 μM, respectively.
In vivo, Rats received PF-562271 demonstrate a decrease in tumor growth after 2 weeks of treatment with signs of bone healing as evidenced by the deposition of new bone (cortical and cancellous) at sites previously damaged by the tumor.
AM J Resp Crit Care. 2018 Mar 26.
Dicer1 deficiency in the IPF fibroblastic focus promotes fibrosis by suppressing microRNA biogenesis
PF-562271 purchased from AbMole
Mol Cancer Ther. 2015 May;1202-12.
Frequent Loss of NISCH Promotes Tumor Proliferation and Invasion in Ovarian Cancer via Inhibiting the FAK Signal Pathway.
PF-562271 purchased from AbMole
 |
Source | AM J Resp Crit Care (2018). Figure E2. PF562271 (Abmole Bioscience) |
| Method | qPCR | |
| Cell Lines | Lung fibroblasts | |
| Concentrations | 10 μM | |
| Incubation Time | 24 h | |
| Results | Focal Adhesion Kinase (PF562271), ALK5 (A83-01), or MTRF (CCG-100602) did not consistently restore fibroblast miR-29 levels on IPF-ECM |
-2.jpg) |
Source | Mol Cancer Ther. (2015) Figure 5. PF-562271 (M2302, Abmole, shanghai, China) |
| Method | western blotting, immunohistochemical staining(IHC) | |
| Cell Lines | SKOV3 cells | |
| Concentrations | ||
| Incubation Time | ||
| Results | NISCH suppressed tumor metastasis via inhibiting FAK signal transduction in vivo. |
-1.jpg) |
Source | Mol Cancer Ther. (2015) Figure 5. PF-562271 (M2302, Abmole, shanghai, China) |
| Method | western blotting, immunohistochemical staining(IHC) | |
| Cell Lines | SKOV3 cells | |
| Concentrations | ||
| Incubation Time | 72h | |
| Results | Nischarin attenuated cell invasion by inhibiting FAK signal transduction. |
| Cell Experiment | |
|---|---|
| Cell lines | MPanc-96 or MAD08-608 cells |
| Preparation method | Cell migration and invasion assays were performed using transwell migration chambers (BD Biosciences, Bedford, MA) as previously described (26–28). Conditioned media was prepared from subconfluent MPanc-96 or MAD08-608 cells by harvesting growth medium (containing 0.5% FBS) for two 24 h periods. The conditioned media was centrifuged to remove cellular debris and concentrated 3 fold using Amicon Ultra-15 3K centrifugal filter devices (Millipore, Billerica, MA). Mock conditioned media was prepared by concentrating 0.5% FBS in similar fashion. For proliferation assays, cells (1.5 × 105) were plated in 96-well plates in 1% FBS-containing media and cell number was measured using the CyQuant assay (Invitrogen, Grand Island, NY). |
| Concentrations | 0~1µM |
| Incubation time | 48h |
| Animal Experiment | |
|---|---|
| Animal models | Orthotopic tumor model (Six-week old male athymic nude mice) |
| Formulation | saline |
| Dosages | 33 mg/kg twice/day |
| Administration | by gastric lavage |
| Molecular Weight | 507.49 |
| Formula | C21H20F3N7O3S |
| CAS Number | 717907-75-0 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related FAK Products |
|---|
| Petunidin chloride
Petunidin chloride is an O-methylated anthocyanidin derived from delphinidin. *The compound is unstable in solutions, freshly prepared is recommended. |
| FAK-IN-11
FAK-IN-11 is a FAK inhibitor. |
| ZINC40099027
ZINC40099027 is a FAK activator. |
| FC-11
FC-11 is a PROTAC FAK degrader (DC90: 1 nM) . |
| FAK-IN-9
FAK-IN-9 is a potent and orally active FAK inhibitor with an IC50 of 27.44 nM. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
