R1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta? FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2.
CL-387785 is an irreversible inhibitor of EGFR with IC50 of 370+/-120 pM; is able to overcome resistance caused by the T790M mutation on a functional level.
AMG-47a is an orally bioavailable potent inhibitor of Lck and T cell proliferation. It exhibits anti-inflammatory activity (ED50 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice.
LDK378 is a highly selective, orally bioavailable and ATP-competitive small molecule inhibitor of ALK (Anaplastic Lymphoma Kinase), a receptor tyrosine kinase considered to be an important lung cancer drug target.
Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.
SB1317 is a potent inhibitor of Cyclin dependent kinases (CDKs), FMS-like tyrosine kinase-3 (FLT3) and Janus kinase 2 (JAK2) with IC50 values of 13nM, 56nM and 73nM for CDK2, JAK2 and FLT3, respectively.
Flumatinib mesylate can reduce the expression of C-MYC, HIF-1 a and VEGF in U266 cell line in a time- and dose-dependent manners, so flumatinib mesylate may become a new drug for MM therapy.
JI-101 is an orally active inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor beta (PDGFRβ), and the ephrin B4 receptor B4 (EphB4) with potential antiangiogenic and antineoplastic activities.
TAK-593 is an oral formulation containing a small-molecule receptor tyrosine kinase inhibitor of both vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with potential antineoplastic activity.
FN-1501 is a potent inhibitor of FLT3 and CDK, with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively. FN-1501 has anticancer activity.
PP1 Analog II, 1NM-PP1 is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors.
AG-1288 is a tyrosine kinase inhibitor. Has been shown in human amnion cells (IC50 =21 mM) to block glucocorticoid-induced cytotoxicity, TNFα-induced cytotoxicity, and glucocorticoid-induced COX-2 activity.
Tyrphostin AG 957 is a potent tyrosine kinase inhibitor. Selectively blocks the tyrosine kinase activity of human p210bcr-abl (Ki = 750 nM) over p140c-abl (Ki = 10 μM).
ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3.
EGFR inhibitor is a cell permeable, 4,6-disubstituted pyrimidine compound that selectively inhibits the EGFR kinase with an IC50 value of 21 nM in vitro and blocks receptor autophosphorylation in cells.
AZD-9291 is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors.
Icotinib hydrochloride is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC(50) of 5 nM, including it's mutants of EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).
GNF-5837 is a potent, selective, and orally bioavailable pan-TRK inhibitor that inhibited tumor growth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF.
R428 is a selective small molecule inhibitor of Axl kinase, which showed activity to blocks tumor spread and prolongs survival in models of metastatic breast cancer.
CEP-28122 is a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers.
CNX-2006 is a potent, mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clinical trial for the treatment of EGFR-mutant lung cancer.
CEP-32496 is an orally available v-raf murine sarcoma viral oncogene homolog B1 (B-raf) serine/threonine protein kinase inhibitor with potential antineoplastic activity.
Epertinib is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib shows potent antitumor activity.
UNC569 is a novel small-molecule MER inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo. UNC569 is the first small-molecule Mer inhibitor. UNC569 inhibited Mer activation and downstream signaling through ERK1/2 and AKT.
CGP77675 is a potent Src kinase inhibitor. CGP77675 inhibited phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50: 5-20 and 40 nM, respectively).
DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine kinase inhibitor with IC50/EC50 of 105 nM/87 nM, 4-fold less potent for DDR2 (IC50= 413 nM).
KU14R is an antagonist of the pancreatic β-cell atypical imidazoline binding site (putative I3 receptor). KU14R has also been shown to selectively block efaroxan-induced insulin secretion.
AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.
