Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor, with potential antiangiogenic and antineoplastic activities. The combination of Defactinib (VS-6063) and paclitaxel synergistically decreases proliferation and increases apoptosis in SKOV3ip1, SKOV3-TR, HeyA8 and HeyA8-MDR cells. In both PTX-sensitive and PTX-resistant models, VS-6063 (50 mg/kg p.o.) enhances tumor growth inhibition by paclitaxel.
| Cell Experiment | |
|---|---|
| Cell lines | BON, QGP-1, and CM cells |
| Preparation method | For MTT assay to assess viability, 3x103 cells per well were seeded in a 96 well plate and allowed to attach overnight then treated with the indicated doses of PF-04554878 for 72 hours prior to the addition of 20 µL of 5 mg/mL MTT in PBS for 4 hours, followed by absorbance reading at 562 nm using a SpectraMax M5 microplate reader. |
| Concentrations | 0.01-100 uM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | Five-week-old male and female NOD.CB17-Prkdc scid/NcrCrl (NOD/SCID) mice |
| Formulation | dissolved in corn oil |
| Dosages | 50 mg/kg daily |
| Administration | oral gavage |
| Molecular Weight | 510.49 |
| Formula | C20H21F3N8O3S |
| CAS Number | 1073154-85-4 |
| Solubility (25°C) | DMSO ≥ 30 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. |
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