|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.|
NVP-ACC789 is a potent, selective and orally active inhibitor of the VEGF receptor tyrosine kinases, antagonizing tumor-driven angiogenesis
E 3810 dihydrochloride is a dual VEGFR/FGFR tyrosine kinase inhibitor. It suppresses the tumor angiogenesis and tumor cell proliferation via inhibiting VEGFR1, ...
BRN-103 can suppress the phosphorylation of vascular endothelial growth factor (VEGF) receptor 2. It can also inhibit the activations of AKT and eNOS. These res...
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.
SU11652 is a cell-permeable and sunitinib-like inhibitor of tyrosine kinase receptor (RTK) and angiogenesis with antineoplastic property. It selectively inhibit...
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...
Vatalanib, also called as PTK 787 or CGP 797870, is a small molecule that interacts reversibly and competitively at the ATP-binding site of the receptor tyrosin...
Fruquintinib, also known as HMPL-013, is an orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential ...
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.
Brivanib alaninate is the alaninate ester of a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with potential antineoplastic activity. Brivanib...
Regorafenib, also known as BAY 73-4506, is an orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. Regorafenib binds ...
Sulfatinib, an oral drug candidate, is a small molecule inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3, and the fibroblast growth...
SU1498 is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 (VEGFR2, aka FLK1; IC50 = 700 nM), and inhibits Flk-1 with an IC50 of value of 7...
A potent, selective and cell-permeable inhibitor of VEGFR2 kinase(IC50= 70 nM) with little or no effect against receptors for platelet-derived growth factor, ep...
SU5402 is a potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor.
Semaxanib, also known as SU5416, is a quinolone derivative with potential antineoplastic activity. Semaxanib reversibly inhibits ATP binding to the tyrosine kin...
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 ...
Cediranib (AZD-2171; tentative trade name Recentin) is a potent inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases.The drug is bei...
Apatinib mesylate is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. Apa...
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.