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Defactinib hydrochloride

Cat. No. M8945
Defactinib hydrochloride Structure
Synonym:

VS-6063 HCl; PF04554878 HCl

Size Price Availability
10mg USD 120 4-7 Days
50mg USD 300 4-7 Days
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 546.95
Formula C20H22ClF3N8O3S
CAS Number 1073160-26-5
Purity >98%
Solubility DMSO: ≥ 25 mg/mL (Need ultrasonic)
Storage at -20°C
References

FAK signaling in human cancer as a target for therapeutics.
Lee BY, et al. Pharmacol Ther. 2015 Feb;146:132-49. PMID: 25316657.

Role of focal adhesion kinase in regulating YB-1-mediated paclitaxel resistance in ovarian cancer.
Kang Y, et al. J Natl Cancer Inst. 2013 Oct 2;105(19):1485-95. PMID: 24062525.

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Defactinib

Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor.

  Catalog
Abmole Inhibitor Catalog 2017




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

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