product name Defactinib (PF-04554878)
Description: Defactinib (also known as VS-6063, PF-04554878) is a potent, selective, and orally bioactive FAK inhibitor. Defactinib has antiangiogenic and antineoplastic activities. FAK inhibitor PF-04554878 inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt, thus inhibiting tumor cell migration, proliferation and survival.
References: J Natl Cancer Inst. 2013 Oct 2;105(19):1485-95; Oncotarget. 2014 Sep 15;5(17):7945-59.
510.49
Formula
C20H21F3N8O3S
CAS No.
1073154-85-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 5 mg/mL (9.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
5% DMSO+50% PEG 300+5% Tween 80+ddH2O: 5mg/mL
Synonyms
VS-6063 and PF-04554878
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19420260
| In Vitro |
In vitro activity: In taxane-sensitive (SKOV3ip1) and taxane-resistant (SKOV3-TR) cell lines, VS-6063 significantly inhibits pFAK (Tyr397) expression. The combination of VS-6063 and paclitaxel synergistically decreases proliferation and increases apoptosis in SKOV3ip1, SKOV3-TR, HeyA8 and HeyA8-MDR cells. The combination of VS-6063 and Y15 synergistically decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines. Kinase Assay: Cell Assay: Ovarian cancer cells are treated with increasing concentrations of VS-6063 for 96 hours and then subjected to the MTT assay. Results are confirmed with triplicate experiments. |
|---|---|
| In Vivo | In both PTX-sensitive and PTX-resistant models, VS-6063 (50 mg/kg p.o.) enhances tumor growth inhibition by paclitaxel. |
| Animal model | Mice bearing SKOV3ip1, SKOV3-TR, HeyA8 or HeyA8-MDR tumors |
| Formulation & Dosage | Dissolved in PBS; 50 mg/kg; Administered through p.o. |
| References | J Natl Cancer Inst. 2013 Oct 2;105(19):1485-95; Oncotarget. 2014 Sep 15;5(17):7945-59. |
