FAK inhibitor 2

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

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.

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.

AT-533 is a potent inhibitor of Hsp90 and HSV. AT-533 blocks the HIF-1α VEGF VEGFR-2 signaling pathway, leading to suppress tumor growth and angiogenesis. AT-533 also inhibits the activation of the downstream pathways, including Erk1 2, FAK, Akt mTOR p70S6K,. AT-533 inhibits the cell migration, invasion, and the tube formation of human umbilical vein endothelial cells (HUVECs).

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

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

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.

FAK-IN-3 is a potent inhibitor of adherens spot kinase (FAK). FAK-IN-3 reduces migration and invasion of PA-1 cells and inhibits the expression of MMP-2 and MMP-9. FAK-IN-3 inhibits tumor growth and metastasis with no significant adverse effects. FAK-IN-3 has shown investigational potential in ovarian cancer.

FAK-IN-2 is a potent, orally active adherens spot kinase (FAK) inhibitor (IC50: 35 nM) that exhibits antitumour effects. FAK-IN-2 covalently inhibits FAK autophosphorylation in a dose-dependent manner and also inhibits tumour cell formation and migration and induces apoptosis.

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.