Kidney cancer is a type of cancer that starts in the kidneys. These organs, positioned on the sides of the abdomen, have the responsibility of filtering waste and excess water from the bloodstream and sending them out in the urine; they are shaped like beans. The most common type of kidney cancer in those of adult age is renal cell carcinoma. In children, the most common type is referred to as Wilms' tumor. It is estimated that over 50,000 people are diagnosed with renal cancer in the United States each year; that number is sure to be higher around the world.
Typically, kidney cancer develops in people who are over 40 years of age. However, it can develop in people who are much younger, and no one knows its exact cause. There are some risk factors that increase kidney cancer risk; they include smoking, obesity, high blood pressure, and years of dialysis. If someone has an abnormal Von Hippel-Lindau (VHL) gene, he is also more likely to develop this type of cancer. People exposed to asbestos and cadmium occupationally may also be more at risk. For some reason, men are diagnosed with kidney cancer more often than women.
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PT2385 (PT-2385) is a potent, selective, and orally active antagonist of HIF2α, binds to HIF2α PAS-B domain (Kd=50 nM) and disrupts HIF2α/ARNT dimer formation; allosterically blocks HIF2α dimerization with the HIF1α/2α transcriptional dimerization partner ARNT/HIF1β, disrupts HIF2α, but not HIF1α, heterodimerization with ARNT in Hep3B cells; inhibits the expression of HIF2α-dependent genes, including VEGF-A, PAI-1, and cyclin D1 in ccRCC cell lines and tumor xenografts, also reduces HIF2α mRNA and protein levels in xenograft tumors.
LY-2510924 (LY2510924) is a potent and selective, cyclic peptide CXCR4 antagonist with IC50 of 0.079 nM, without apparent agonist activity; inhibits SDF-1-induced cell migration with IC50 of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling; exhibits inhibition of SDF-1-stimulated phospho-ERK and phospho-Akt in tumor cells; shows inhibition of tumor growth in human xenograft models with acceptable in vivo stability and a pharmacokinetic profile.
STF-62247 is a small molecule Autophagy inducer that induces autophagy and selectively induces lethality in VHL-deficient RCC cells; induces cytotoxicity and reduces tumor growth in VHL-deficient cells in a HIF-independent manner, PI3K and Golgi trafficking are required as initial signals in STF-62247-induced autophagy.
Tivozanib is a highly potent inhibitor of pan-VEGFR with IC50s of 60/6.5/15 nM for VEGFR1/2/3; also inhibits EphB2, PDGFR-α, PDGFR-β, c-Kit, and Tie2 (IC50=20-80 nM); inhibits VEGF-induced VEGFR-2 phosphorylation in endothelial cells (IC50=0.16 nM); p.o. active.
Cabozantinib (XL184) is a potent, multi-kinase inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50 of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively; eliminates tumor vasculature, reduces pericytes and empty basement membrane sleeves, causes widespread intratumoral hypoxia and tumor cell apoptosis, and slows regrowth of the tumor vasculature, also decreases invasiveness of primary tumors and reduces metastasis in pancreatic islet cancer; exerts marked anti-MPNST effects in vitro and in vivo.
Pazopanib is a potent, orally available, pan-VEGFR inhibitor with IC50 of 10, 30, and 47 nM for VEGFR-1, -2, and -3, respectively; also shows significant activity against the closely related RTKs PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50 of 84, 74, 140, and 146 nM, respectively; potently inhibits VEGF-induced phosphorylation of VEGFR-2 in HUVEC cells with IC50 of 8 nM; inhibits in vivo tumor growth, increases MM cell apoptosis, decreases angiogenesis, and prolongs host survival in a xenograft model of human MM.
Pazopanib hydrochloride is a potent, orally available, pan-VEGFR inhibitor with IC50 of 10, 30, and 47 nM for VEGFR-1, -2, and -3, respectively; also shows significant activity against the closely related RTKs PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50 of 84, 74, 140, and 146 nM, respectively; potently inhibits VEGF-induced phosphorylation of VEGFR-2 in HUVEC cells with IC50 of 8 nM; inhibits in vivo tumor growth, increases MM cell apoptosis, decreases angiogenesis, and prolongs host survival in a xenograft model of human MM.
Lenvatinib (E7080) is a multitargeted kinase inhibitor with IC50s of 4/5.2/22/46 nM for VEGFR2/VEGFR3/VEGFR1/FGFR1 in cell free assays; also inhibits PDGFR, Kit with IC50< 100 nM; suppresses the phosphorylation of VEGF receptor-2 and FGF receptor 1 and inhibits proliferation of endothelial cellin vitro; orally active.
CB-839 (Telaglenastat) is a potent, selective, and orally bioavailable inhibitor of glutaminase with IC50 of 28 and 23 nM for glutaminase in kidney and brain (GAC and KGA), but not the liver form of glutaminase (GLS2, IC50>1 uM); demonstrates antiproliferative activity in triple-negative breast cancer (TNBC) cell line HCC-1806 and MDA-MB-231 with IC50 of 20-55 nM, decreases glutamine consumption, glutamate production, oxygen consumption, and the steady-state levels of glutathione and several tricarboxylic acid cycle intermediates; exhibits vivo efficacy in breast cancer xenograft models, both as a single agent and in combination with paclitaxel.
Sorafenib is a potent, orally available Raf inhibitor with IC50 of 6, 22, and 38 nM for Raf-1, wt Braf, and BRaf V599E, respectively; Also demonstrates potent inhibition of certain proangiogenic RTKs, including VEGFR-2, PDGFR-β, VEGFR-3, Flt-3, c-Kit (IC50<100 nM); Exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.
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