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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $31 | In Stock | |
2 mg | $41 | In Stock | |
5 mg | $67 | In Stock | |
10 mg | $87 | In Stock | |
25 mg | $153 | In Stock | |
1 mL x 10 mM (in DMSO) | $75 | In Stock |
Description | Defactinib (VS-6063) is an orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. |
In vitro | In both paclitaxel-sensitive and paclitaxel-resistant models, oral administration of VS-6063 (50 mg/kg) was able to induce growth inhibitory effects. |
In vivo | In both paclitaxel-sensitive (SKOV3ip1) and paclitaxel-resistant (SKOV3-TR) cell lines, VS-6063 inhibits the expression of pFAK (Tyr397). In thyroid cancer cell lines, the combined application of VS-6063 and Y15 effectively suppresses cell adhesion and proliferation. Furthermore, in the cell lines SKOV3ip1, SKOV3-TR, HeyA8, and HeyA8-MDR, a synergistic effect between VS-6063 and paclitaxel significantly reduces cell proliferation and induces apoptosis. |
Kinase Assay | Cell-free Kinase Activity Assays: IC50 values for TG101348 are determined commercially using the InVitrogen kinase profiling service for a 223 kinase screen that included JAK2 and JAK2V617F or Carna Biosciences for the screen of all Janus kinase family members including JAK1 and Tyk2. ATP concentration is set to approximately the Km value for each kinase. |
Cell Research | 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.(Only for Reference) |
Alias | PF-04554878, VS-6063 |
Molecular Weight | 510.49 |
Formula | C20H21F3N8O3S |
Cas No. | 1073154-85-4 |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (97.94 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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