FAK

Ifebemtinib (BI-853520) is an orally active and potent inhibitor of adhesion plaque kinase (FAK) (IC50=1 nM) with anti-tumour activity that inhibits globule formation and in situ tumour growth in malignant pleural mesotheliomas, and may be useful for the study of breast and ovarian cancer.

Ifebemtinib FA (BI-853520 FA) is an orally active and potent inhibitor of adhesion patch kinase (FAK) with anticancer and antiproliferative activity for the study of ovarian and lung cancer.

Compound 1T-0219 (SC) is a blocker of AKT1-FAK interaction reducing the stimulation of FAK phosphorylation in response to extracellular pressure in human SW620 colon cancer cells without affecting basal FAK phosphorylation.

Conteltinib (CT-707) is an enzyme inhibitor with antitumor activity targeting FAK, ALK, and Pyk2.Conteltinib exhibits significant inhibition of FAK, overcomes hypoxia-mediated sorafenib resistance in hepatocellular carcinoma through inhibition of YAP signaling, and can be used in advanced ALK-positive non-small-cell lung cancer and lymphoma.

Roslin 2 bromide (Benzylhexamethylenetetramine bromide) is a p53 reactivator that disrupts the binding of FAK and p5. Roslin 2 bromide exhibits anticancer effects.

ZINC40099027 is a specific adhesion plaque kinase (FAK) activator that promotes gastric mucosal repair in persistent aspirin-associated gastric injury through activation of adhesion plaque kinase, activates human adhesion plaque kinase by accelerating the enzyme activity of the structural domain of FAK kinase, activates cytosolic FAK, and promotes intestinal epithelial wound closure.

PF-573228 is an ATP-competitive FAK inhibitor. In a cell-free assay, the IC50 of FAK is 4 nM.

Y15 (1,2,4,5-Benzenetetramine tetrahydrochlor) is a potent and specificsmall-molecule FAK scaffolding inhibitor that inhibits its autophosphorylation activity, blocks tumor growth.

5alpha-Hydroxycostic acid possesses anti-angiogenic ability by interfering the VEGF- and Ang2-related pathways, and it may be a good drug candidate.

NVP-TAE 226 (TAE226) is an effective FAK inhibitor (IC50: 5.5 nM) and most effective to Pyk2(IC50: 3.5 nM); 10- to 100-fold less effective against IGF-1R, InsR, c-Met, and ALK.

PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).

Defactinib (VS-6063) is an orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities.

GSK2256098 (GTPL7939) is a small molecule FAK kinase inhibitor.

PF-431396 is a dual PYK2/FAK inhibitor (IC50: 11/2 nM).

Compound 2119738-71-3 interacts with the FAK receptor.

ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A shows comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability.Excisanin A induces apoptosis in colon cancer cell line SW620 as determined by Annexin V staining, the cleavage of caspase-3 and the proteolytic degradation of poly (ADP-ribose) polymerase (PARP).

FAK-IN-7 has potential antiproliferative activity and is a FAK inhibitor.

FAK-IN-12 (Compound 12S) is a selective FAK inhibitor with an IC50 of 47 nM. It effectively suppresses proliferation of MGC-803, HCT-116, and KYSE30 cells with IC50 values of 0.24, 0.45, and 0.44 μM, respectively. Additionally, FAK-IN-12 promotes apoptosis and cellular senescence [1].

FAK-IN-11 (Compound 4l), a FAK inhibitor, specifically targets the ATP binding pocket of FAK to prevent its phosphorylation. It exhibits cytotoxic effects on MDA-MB-231 cells, achieving an IC50 value of 13.73 μM, and induces non-apoptotic cell death in these cells [1].

FAK-IN-10 is an inhibitor of FAK (IC50:76.3 μM).FAK-IN-10 z MCF-7 and A431 cell lines showed antitumor activity with IC50 of 4.23 and 0.78 μM, respectively.

Masitinib mesylate (AB-1010 mesylate) is a selective and orally bioavailable c-Kit inhibitor (IC50 of 200 nM,540/800 nM,510 nM for human recombinant c-Kit;PDGFRα/β;LynB,respectively).

CEP-37440 is an effective and specific Dual FAK/ALK inhibitor with IC50s of 120 nM(ALK cellular in 75% human plasma) and 2.3 nM (FAK).

ALK inhibitor 1 is a selective ALK kinase inhibitor.

Corosolic acid (Colosic acid) contains anti-angiogenic activity that can suppress FAK signaling induced by angiopoietin-1. Corosolic acid exerts anticancer activities against HCC, colon, and colorectal Y cells, by inducing apoptosis and promoting the N-terminal phosphorylation and subsequent proteasomal degradation of β-catenin.

Inulicin (1-O-Acetylbritannilactone), an active compound isolated from Inula Britannica L, inhibits VEGF-mediated activation of Src and FAK.

YH-306 (TRV055 acetate ) is a modulator of the FAK signaling pathway that acts by suppressing colorectal tumor growth and metastasis.

Masitinib (AB1010) is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet and has been available for veterinaries since 2011.

PF-562271 hydrochloride (PF-562271 HCl) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.

(R)-Fangchinoline ((+)-Thalrugosine) is extracted from Stephania tetrandra S. Moore.

FAK inhibitor 2, antitumor and anti-angiogenesis activitiesis ,is a potent focal adhesion kinase (FAK) inhibitor with an IC50 of 0.07 nM .

AMP-945 is a proprietary focal adhesion kinase (FAK) inhibitor.

BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM. A PTK2 ligand for PROTAC

PF-562271 besylate (PF-00562271 Besylate) 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.

PF-03814735 is a novel, potent and reversible inhibitor of Aurora A B with IC50of 0.8 nM 5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.

Batatasin III inhibits cancer migration and invasion by suppressing epithelial to mesenchymal transition and FAK-AKT signals and possesses anti-cancer activities. Batatasin III has a long-term inhibitory effect on whole-plant growth and shows germination

SU 6656 is a selective inhibitor of Src family kinases, with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.

ALK inhibitor 2 is a new-type and selective inhibitor for the ALK kinase.

Chloropyramine hydrochloride (Alergosan) is a histamine receptor H1 antagonist.

1. Nitidine chloride has inhibitory effects on various tumors, such as renal cancer , breast cancer. 2. Nitidine chloride inhibits the proliferation of SMMC-7721 cells in vitro in a time- and dose-dependent manner and identifies efficacy in vivo in a mouse model of HCC.

NAMI-A is a ruthenium-based compound with selective activity against tumor metastasis.NAMI-A inhibits cancer cell adhesion and migration.

GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader (pDC50= 8.4). GSK215 is designed by the FAK inhibitor VS-4718 and a binder for the VHL E3 ligase. GSK215 can induce rapid and prolonged FAK degradation.

AZ7550, an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).

Fangchinoline (Tetrandrine B) is extracted from Stephania tetrandra S. Moore.

Defactinib hydrochloride (PF 04554878 hydrochloride) is a novel inhibitor of FAK. Which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.

BMS-536924 (BMS 536924) is an ATP-competitive IGF-1R IR inhibitor with IC50 of 100 nM 73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1 2.

PND-1186 (VS-4718) is a reversible and specific FAK inhibitor (IC50: 1.5 nM).