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Defactinib hydrochloride

Cat. No. M8945

All AbMole products are for research use only, cannot be used for human consumption.

Defactinib hydrochloride Structure
Synonym:

VS-6063 HCl; PF04554878 HCl

Size Price Availability
10mg USD 120  USD120 4-7 Days
50mg USD 300  USD300 4-7 Days
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
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
Chemical Information
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
References

[1] Lee BY, et al. Pharmacol Ther. FAK signaling in human cancer as a target for therapeutics.

[2] Kang Y, et al. J Natl Cancer Inst. Role of focal adhesion kinase in regulating YB-1-mediated paclitaxel resistance in ovarian cancer.

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  Catalog
Abmole Inhibitor Catalog




Keywords: Defactinib hydrochloride, VS-6063 HCl; PF04554878 HCl supplier, FAK, inhibitors, activators

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