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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.

Kidney Cancer

Phase 2 Clinical




OBP-801 (YM 753;Spiruchostatin A) is a novel cyclic-peptide-based HDAC inhibitor with IC50 of 2 nM; significantly inhibits the cell growth on comparison with each agent alone and synergistically increased apoptosis with the induction of Bim; significantly suppresses tumor growth in vivo.

Kidney Cancer

Phase 1 Clinical




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.

Kidney Cancer

Phase 2 Clinical




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.

Kidney Cancer





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.

Kidney Cancer




849217-68-1 Cabozantinib (XL184, BMS-907351) 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.

Kidney Cancer




1672665-49-4 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.

Kidney Cancer

Phase 2 Clinical

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