ptk2/fak

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

Defactinib (VS-6063) is a second-generation inhibitor of FAK that inhibits FAK phosphorylation at the Tyr397 site. Defactinib has potential antitumor activity.

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.

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

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

NVP-TAE 226 (TAE226) is a potent FAK inhibitor (IC50: 5.5 nM), exhibiting even greater efficacy against Pyk2 (IC50: 3.5 nM), and is 10- to 100-fold less effective against IGF-1R, InsR, c-Met, and ALK.

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

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

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

ALK inhibitor 1 is a selective ALK kinase inhibitor.

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.

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.

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

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

Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) is a PROTAC linker characterized by its PEG composition, crucial in synthesizing various PROTACs, including BI-3663, a selective PTK2 FAK PROTAC. Using cereblon ligands, it targets E3 ligases to degrade PTK2, exhibiting potent inhibitory activity with an IC50 of 18 nM[1].

BI-3663 is a highly selective PTK2 FAK PROTAC that utilizes cereblon ligands to hijack E3 ligases for PTK2 degradation, with an IC50 of 18 nM. It is composed of BI-4464 linked to Pomalidomide with a linker[1]. Anti-cancer.

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.

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

BI-4464, a highly selective ATP-competitive inhibitor of PTK2 FAK, exhibits an IC50 of 17 nM and serves as a PTK2 ligand for PROTAC (Proteolysis Targeting Chimera).

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.

TAK-960 hydrochloride is a potent, selective, orally active inhibitor of polo-like kinase 1 (PLK1) (IC50: 0.8 nM). TAK-960 hydrochloride inhibits the proliferation of a variety of tumour cell lines and significantly treats a variety of tumour xenografts.

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.