Defactinib hydrochloride inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner, which may prevent the integrin-mediated activation of several downstream signal transduction pathways. RPPA data shows that VS-6063 reduces levels of AKT and YB-1 in taxane-resistant cell lines.
In vivo, Defactinib hcl doses of 25 mg/kg twice a day or greater statistically significantly inhibits pFAK (Tyr397) at 3 hours, with return of expression noted by 24 hours.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Mice |
| Formulation | prepared in phosphate-buffered saline |
| Dosages | 25 mg/kg twice every day |
| Administration | orally |
| Molecular Weight | 546.95 |
| Formula | C20H22ClF3N8O3S |
| CAS Number | 1073160-26-5 |
| Solubility (25°C) | DMSO: ≥ 25 mg/mL (Need ultrasonic) |
| 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.
[1] Lee BY, et al. Pharmacol Ther. FAK signaling in human cancer as a target for therapeutics.
| 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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