|Description||KRN633 is a potent and selective VEGFR inhibitor. which inhibits tyrosine phosphorylation of VEGFR-2 (IC50 = 1.16 nmol/L) in human umbilical vein endothelial cells. Selectivity profiling with recombinant tyrosine kinases showed that KRN633 is highly selective for VEGFR-1, -2, and -3. KRN633 inhibits tumor growth in several in vivo tumor xenograft models with diverse tissue origins, including lung, colon, and prostate, in athymic mice and rats. KRN633 also causes the regression of some well-established tumors and those that had regrown after the cessation of treatment. KRN633 was well tolerated and had no significant effects on body weight or the general health of the animals. KRN633 might be useful in the treatment of solid tumors and other diseases that depend on pathologic angiogenesis.|
|Synonyms||KRN633; KRN-633; KRN 633.|
Vandetanib is an anti-cancer drug that is used for the treatment of certain tumours of thethyroid gland. It acts as a kinase inhibitor of a number of cell recep...
Fruquintinib, also known as HMPL-013, is an orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential ...
Tyrphostin 9 is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM.
Semaxanib, also known as SU5416, is a quinolone derivative with potential antineoplastic activity. Semaxanib reversibly inhibits ATP binding to the tyrosine kin...
Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4.
2,4-Pyrimidinediamine with linker
2,4-Pyrimidinediamine with linker is a patent compound in WO2013055780A1, Page 71; multikinase inhibitor and has a -NH2 terminal linker for further synthesis.
BAW 2881 is a VEGFR (vascular endothelial growth factor receptor) inhibitor (IC50 = 0.82, 0.037, and 0.42 µM for VEGFR1, 2, and 3, respectively).It can inhibit ...
Brivanib is the hydrolyzed form of Brivanib alaninate, which is a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with potential antineoplastic...
SAR131675 dose dependently inhibits the proliferation of primary human lymphatic cells, induced by the VEGFR-3 ligands VEGFC and VEGFD, with an IC50 of about 20...
axitinib is an orally bioavailable tyrosine kinase inhibitor. Axitinib inhibits the proangiogenic cytokines vascular endothelial growth factor (VEGF) and platel...
SKLB1002 is a new potent VEGFR2 inhibitor, which could significantly inhibit HUVEC proliferation, migration, invasion, and tube formation. In vivo zebrafish mo...
Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM.
Cabozantinib malate (XL184)
Cabozantinib malate is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL w...
Regorafenib monohydrate is a multitargetedinhibitor of tyrosine kinase with IC50 values of 13nM, 4.2nM, 46nM, 2.5nM, 28nM, 19nM, 202nM, 22nM, 7nM, 1.5nM and 311...
Cabozantinib is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 1...
AG28262 is a bio-active chemical compound. It is a VEFG-r2 inhibitor and could cause an increase in serum ALT, due in part to both gene up-regulation.
Tivozanib is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplast...
TG 100801 Hydrochloride
TG 100801 is the prodrug of TG 100572, which is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kin...
Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more s...
Regorafenib, also known as BAY 73-4506, is an orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. Regorafenib binds ...