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Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor, with potential antiangiogenic and antineoplastic activities. The combination of Defactinib (VS-6063) and paclitaxel synergistically decreases proliferation and increases apoptosis in SKOV3ip1, SKOV3-TR, HeyA8 and HeyA8-MDR cells. In both PTX-sensitive and PTX-resistant models, VS-6063 (50 mg/kg p.o.) enhances tumor growth inhibition by paclitaxel.
J Gastroenterol Hepatol. 2024 Oct 15.
The m6A reader IGF2BP1 contributes to the activation of hepatic stellate cells through facilitating TUBB4B mRNA stabilization
Defactinib purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | BON, QGP-1, and CM cells |
| Preparation method | For MTT assay to assess viability, 3x103 cells per well were seeded in a 96 well plate and allowed to attach overnight then treated with the indicated doses of PF-04554878 for 72 hours prior to the addition of 20 µL of 5 mg/mL MTT in PBS for 4 hours, followed by absorbance reading at 562 nm using a SpectraMax M5 microplate reader. |
| Concentrations | 0.01-100 uM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | Five-week-old male and female NOD.CB17-Prkdc scid/NcrCrl (NOD/SCID) mice |
| Formulation | dissolved in corn oil |
| Dosages | 50 mg/kg daily |
| Administration | oral gavage |
| Molecular Weight | 510.49 |
| Formula | C20H21F3N8O3S |
| CAS Number | 1073154-85-4 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related FAK Products |
|---|
| NVP-TAE226
Nvp-tae 226 (TAE226) is a potent atP-competitive dual FAK and IGF-1R inhibitor with IC50 of 5.5 nM and 140 nM, respectively. Nvp-tae 226 (TAE226) also effectively inhibited Pyk2, insulin receptor (InsR), with IC50 of 3.5 nM and 40 nM. |
| PF-562271
PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively. |
| PF-573228
PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. |
| PF-00562271
PF-00562271 is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. |
| PND-1186
PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. |
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Products are for research use only. Not for human use. We do not sell to patients.
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