ASP3026 is a novel and selective inhibitor for the ALK kinase. ASP3026 potently inhibited ALK kinase activity and was more selective than crizotinib in a Tyr-kinase panel.
ALK-IN-1, an analog of AP26113, is an orally-available, potent, and selective inhibitor of ALK with a potency of 0.62 nM against wild-type and activity against a wide range of mutants, including the crizotinib-resistant L1196M line.
Thalidomide fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.
Scutellarin, a main active ingredient extracted from Erigeron breviscapus (Vant.) Hand-Mazz, has been wildly used to treat acute cerebral infarction and paralysis induced by cerebrovascular diseases.
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.
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.
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).
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.
Lorlatinib (PF-06463922) is a potent, dual ALK/ROS1 inhibitor with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively.
