Protein Tyrosine Kinases

Neratinib (HKI-272) is a tyrosine kinase inhibitor.

XL184 free base (Cabozantinib) is a small molecule designed to inhibit multiple receptor tyrosine kinases, specifically MET and VEGFR2.

E7080 is a multi-kinase inhibitor that inhibits both VEGFR2 and VEGFR3 kinases.

Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively.

Nintedanib is a potent inhibitor of multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs).

OSI-906 is a potential first-in-class selective small molecule, dual kinase inhibitor of both insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR).

Toceranib is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ.

AG 490 is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). Also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.

Osimertinib (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.

Gilteritinib is a potent FLT3/AXL inhibitor, which showed potent antileukemic activity against AML with either or both FLT3-ITD and FLT3-D835 mutations.

(-)-Catechin gallate is an antioxidant constituent of green tea. At uM concentrations, inhibits VEGF-induced tyrosine phosphorylation.

Crenolanib (CP-868596) is an orally bioavailable, selective small molecule inhibitor of the PDGFR tyrosine kinase, inhibiting both PDGFRA and PDGFRB at picomolar concentrations.

Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway. Lapatinib is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.

SU 5416 is an inhibitor of vascular endothelial growth factor receptor (VEGFR) that also inhibits other tyrosine kinases KIT, MET, FLT3 and RET.

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.

Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.

BMS-536924 is an effective inhibitor of IGF-IR, causing a reversion of an IGF-IR - mediated transformed phenotype.

GW2580 is a small-molecule, ATP-competitive inhibitor of cFMS kinase.

Imatinib (Gleevec) is a number of tyrosine kinase enzymes specific inhibitor.

Pexidartinib is a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity.

Fexagratinib (AZD4547) is a potent, selective and orally active pan-FGFR inhibitor, with IC50s of 0.2, 2.5, 1.8 and 165 nM for FGFR1, 2, 3 and 4, respectively.

NVP-BHG712 is a selective inhibitor of EphB4 kinase that exhibits selectivity for EphB4 over more than 40 other kinases in vitro, including FGFR3.

Masitinib (AB1010) is a protein tyrosine kinase inhibitor.

The ITK inhibitor BMS-509744 disrupts several aspects of HIV replication.

PLX5622 is a highly selective brain penetrant and oral active CSF1R inhibitor with an Ki of 5.9 nM, for extended and specific microglial elimination, preceding and during pathology development.

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.

Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively.

PF-2341066 (Crizotinib) is an inhibitor of the c-Met kinase and the NPM-ALK. PF-2341066 inhibited cell proliferation in ALK-positive ALCL cells (IC50s=30 nM).

Pelitinib (EKB-569) is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity.

R406 is an orally available spleen tyrosine kinase inhibitor with an IC50 of 41 nM.

(-)-Epigallocatechin gallate is a potent anti-oxidant polyphenol flavonoid isolated from green tea.

BIBW2992 (Afatinib) is tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases.

Sunitinib is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST).

Axitinib is a small molecule tyrosine kinase inhibitor,which inhibits multiple targets, including VEGFR-1, VEGFR-2, VEGFR-3, platelet derived growth factor receptor (PDGFR), and cKIT (CD117).

AC220 (Quizartinib) is a uniquely potent and selective FLT3 inhibitor with IC50 of 0.56±0.3 nM and >10 mM for MC4-11 and A375, respectively.

Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.

BGJ398 is a potent and selective inhibitor with potential antiangiogenic and antineoplastic activities of fibroblast growth factor receptor (FGFR) tyrosine kinases 1, 2, 3 and 4 (with IC50 values of 0.9, 1.4, 1.0 and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4 respectively).

AZD8931 is an oral, equipotent inhibitor of ErbB1, ErbB2 and ErbB3 receptor signaling.

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.

DMH-1 is a selective inhibitor of the bone morphogenic protein (BMP) ALK2 receptor (IC50 = 108 nM).

AP24534 (Ponatinib) is a potent multi-kinase and pan-BCR-ABL inhibitor.

Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2

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.

NVP-TAE226 is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2(IC50=3.5 nM); 10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met.

DM1-SMCC is DM1 with a reactive linker SMCC, which can react with antibody to make antibody drug conjugate.

ARQ-197 is a selective inhibitor of the c-Met receptor tyrosine kinase

GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and the insulin receptor with IC50s of 2.0 and 1.6 nmol/L, respectively.

Ki 20227 is an inhibitor of c-Fms tyrosine kinase (M-CSFR, CSF1R).

Apatinib (YN968D1) is a tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor-2 (VEGFR2, also known as KDR) that inhibits VEGF-mediated endothelial cell migration and proliferation thus blocking new blood vessel formation in tumor tissue.

BIBF1120 (Vargatef) is a novel triple angiokinase inhibitor that inhibits three growth factor receptors simultaneously: VEGFR, PDGF and FGFR.