PF 04554878 hydrochloride
PF 04554878 hydrochloride Basic information
- Product Name:
- PF 04554878 hydrochloride
- Synonyms:
-
- Defactinib hydrochloride
- PF 04554878 hydrochloride
- PF04554878 hydrochloride
- PF-04554878 hydrochloride
- VS 6063 hydrochloride
- VS6063 hydrochloride
- VS-6063 hydrochloride
- Defactinib( VS-6063,PF-04554878 ) hydrochloride
- CAS:
- 1073160-26-5
- MF:
- C20H22ClF3N8O3S
- MW:
- 546.95
- Product Categories:
-
- API
- Mol File:
- 1073160-26-5.mol
PF 04554878 hydrochloride Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO:30.0(Max Conc. mg/mL);54.85(Max Conc. mM)
- form
- Solid
- color
- White to off-white
- InChIKey
- RCHQNUQAHJNRBY-UHFFFAOYSA-N
- SMILES
- N(C1=NC(NC2C=CC(C(=O)NC)=CC=2)=NC=C1C(F)(F)F)CC1=NC=CN=C1N(C)S(=O)(=O)C.Cl
PF 04554878 hydrochloride Usage And Synthesis
Uses
Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.
in vivo
Defactinib (VS-6063) 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. Therefore, administration of Defactinib at 25 mg/kg twice a day is selected as the dosing schedule for subsequent therapy experiments. For therapy experiments, female nude mice bearing HeyA8 tumors in the peritoneal cavity are randomly divided into 4 groups (n=10 per group): 1) vehicle orally twice daily and phosphate-buffered saline intraperitoneally weekly (control); 2) Defactinib 25 mg/kg orally twice daily; 3) PTX intraperitoneally weekly; and 4) both VDefactinib 25 mg/kg orally twice daily and PTX intraperitoneally weekly. There is an 87.4% reduction in tumor weight by PTX monotherapy in the HeyA8 model, and combination therapy resulted in the greatest tumor weight reduction, with a 97.9% reduction (P=0.05 compared with PTX). In the SKOV3ip1 model, a 92.7% tumor weight reduction is observed in the combination group compared with PTX (P<0.001)[1].
References
[1] Kang Y, et al. Role of focal adhesion kinase in regulating YB-1-mediated resistance in ovarian cancer. J Natl Cancer Inst. 2013 Oct 2;105(19):1485-95. DOI:10.1093/jnci/djt210
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