Defactinib HCl (formerly known as VS-6063 HCl, PF-04554878 HCl) is a novel, potent, selective, and orally bioactive small molecule inhibitor of the FAK (focal adhesion kinase), it inhibits the phosphorylation of FAK at the Tyr397 site in a time- and dose-dependent manner.
Y11 (Y-11) is a novel and potent small molecule inhibitor of FAK (focal adhesion kinase) with potential anticancer activity.
GSK2256098 is a small molecule developed by GlaxoSmithKline) as a selective FAK (Focal Adhesion Kinase) kinase inhibitor to inhibit FAK activity through targeting the phosphorylation site of FAK, tyrosine (Y) 397.
BI-4464 is a novel, potent and highly selective ATP competitive inhibitor of PTK2/FAK with an IC50 of 17 nM.
Y15 (also known as FAK inhibitor Y15 and FAK Inhibitor 14) is a novel, potent, specific and direct inhibitor of focal adhesion kinase (FAK) which blocks phosphorylation of Y397 with an IC50 value of about 1 μM.
PF-00562271 besylate (also called PF562271 or PF-562271 Besylate), the benzenesulfonate salt form of PF-00562271, is an ATP-competitive and orally bioavailable inhibitor of FAK (focal adhesion kinase) and Pyk2 catalytic activity with potential antitumor activity. It inhibits FAK and Pyk2 with IC50s of 1.5 and 14 nmol/L, respectively. It demonstrates high in vivo antitumor efficacy against […]
PF-562271 is a novel, potent, ATP-competitive, orally bioavailable, reversible inhibitor of FAK (focal adhesion kinase) and Pyk2 catalytic activity with a IC50 of 1.5 and 14 nmol/L, respectively. it has >100-fold selectivity against other protein kinases. Additionally, PF-562,271 displayed robust inhibition in an inducible cell-based assay measuring phospho-FAK with an IC(50) of 5 nmol/L. PF-562,271 […]
PF-573228 (PF573228) is a selective and ATP-competitive FAK (focal adhesion kinase) inhibitor with potential antitumor activity. It inhibits FAK with an IC50 of 4 nM in a cell-free assay, and is ~50- to 250-fold more selective for FAK over other kinases including Pyk2, CDK1/7 and GSK-3β. PF-573228 shows high in vivo antitumor efficacy in PC3M-luc-C6 […]
PF-562271 HCl is the hydrochloride salt of PF-562271 (PF562271 or PF 562271), which is a potent, ATP-competitive, orally bioavailable, reversible inhibitor of FAK (focal adhesion kinase) and Pyk2 (proline-rich tyrosine kinase) catalytic activity with potential anticancer activity. It inhibits FAK and Pyk2 with IC50s of 1.5 and 14 nmol/L, respectively. PF-562271 exhibits >100-fold selectivity for […]
Defactinib (formerly known as VS-6063, PF-04554878) is a selective, ATP-competitive and orally bioactive small molecule inhibitor of the FAK (focal adhesion kinase) with potential antitumor activity. It inhibits the phosphorylation of FAK at the Tyr397 site in a time- and dose-dependent manner. FAK is a nonreceptor tyrosine kinase that plays a vital role in many […]