renal cell carcinoma

Axitinib (AG-013736) is a multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1, VEGFR2, VEGFR3, and PDGFRβ (IC50=4 20 0.4 2 nM). Axitinib has antitumor activity and is used in the treatment of renal cell carcinoma.

Belzutifan (MK-6482) is a potential treatment for clear cell renal cell carcinoma (ccRCC). Belzutifan is an orally active and selective HIF-2α inhibitor (IC50: 9 nM). Belzutifan , as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile.

Nivolumab is a monoclonal antibody, a humanized IgG4 antibody to PD-1. Nivolumab has antitumor activity and is used in the treatment of melanoma, non-small cell lung cancer, renal cell carcinoma and others.

Sparfosic Acid (Acide sparfosique) is an aspartate carbamoyltransferase inhibitor with antitumor activity and can be used to study advanced renal cell carcinoma.

N-Desethyl Sunitinib (SU012662) is the primary active metabolite of Sunitinib produced by the metabolism of cytochrome P450 enzyme 3A4 (CYP3A4).Sunitinib is an orally available inhibitor of a number of tyrosine kinases involved in tumor proliferation and angiogenesis, including VEGFR, PDGFR, KIT, and FLT3, and was approved for the treatment of advanced metastatic renal cell carcinoma (RCC)

ROC-325 is an effective and orally active inhibitor of autophagy with anticancer activity. ROC-325 induces renal cell carcinoma apoptosis and exhibits favorable selectivity.

Apitolisib (RG 7422), an effective, class I PI3K inhibitor for PI3Kα(IC50=5 nM), PI3Kβ(IC50=27 nM), PI3Kδ(IC50=7 nM), PI3Kγ (IC50=14 nM), is used in trials study of solid cancers, breast cancer, prostate cancer, renal cell carcinoma, and endometrial carcinoma, among others.

HC-5404-Fu is an inhibitor of PERK with anti-tumor activity. This compound inhibits the signaling pathway of the endoplasmic reticulum stress response. Additionally, HC-5404-Fu increases the sensitivity of renal cell carcinoma cells to vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitors (TKIs). It holds potential for research into renal cell carcinoma, stomach cancer, metastatic breast cancer, small cell lung cancer, and other solid tumors.

SBI-183 is an orally active QSOX1 inhibitor (Kd: 20 μM). It can inhibit the proliferation and invasion phenotypes of renal carcinoma cell lines, triple-negative breast cancer cell lines, lung adenocarcinoma cell lines, and pancreatic ductal adenocarcinoma. In vivo, SBI-183 suppresses tumor growth in two human renal cell carcinoma xenograft mouse models.

BET Aurora kinase-IN-1 (Compound 38) is a dual inhibitor of BET and Aurora kinases. It exhibits antiproliferative activity against various tumor cell lines and demonstrates significant antitumor efficacy in xenograft models of renal cell carcinoma and colon cancer, with tumor growth inhibition (TGI) rates of 45.99% and 53.06%, respectively.

Tivozanib (KRN951) is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities.

Razoxane is used as an antimitotic agent with immunosuppressive properties.

Phosphostim, a gamma9deta2 T lymphocytes agonist, is used potentially for the treatment of renal cell carcinoma, HCV infection.

CP-461 (OSI-461) is a pde2a 5A inhibitor, which may be used in the treatment of renal cell carcinoma, prostate cancer, and Crohn's disease.

Gramicidin A is a peptide antibiotic isolated from B. brevis.Gramicidin A is a highly hydrophobic channel-forming ion carrier that forms monovalent cation-permeable channels in artificial membranes.Gramicidin A induces the degradation of hypoxia-inducible factor 1 alpha (HIF-1 alpha) and reduces the growth of a mouse xenograft model of human renal cell carcinoma. Gramicidin A has antibacterial, antimalarial and hemolytic activities.

C16 globotriaosylceramide is an endogenous sphingolipid found in mammalian cell membranes that is synthesized from C16 lactosylceramide . C16 globotriaosylceramide acts as a receptor for Shiga toxin in B cell-derived Raji cells and THP-1 monocytes. It accumulates in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease. C16 globotriaosylceramide is also upregulated in plasma of patients with ovarian carcinoma compared to those with benign ovarian tumors or uterine fibroids.

HIF-1 2α-IN-1, an orally active compound, functions as an inhibitor of HIF-2α. Its inhibitory effect on HIF-2α activity is significant, with an IC 50 value of 0.92 μM. Furthermore, HIF-1 2α-IN-1 has the ability to decrease HIF-1α levels. This compound is particularly valuable for research on clear cell renal cell carcinoma (ccRCC) [1].

PERK-IN-5 is a highly selective, potent, orally active inhibitor of protein kinase R-like endoplasmic reticulum (ER) kinase (PERK), displaying inhibition with IC50 values of 2 nM for PERK and 9 nM for p-eIF2α. PERK-IN-5 significantly inhibited tumor growth in the 786-O renal cell carcinoma xenograft tumor model.

STF-62247 is TGN inhibitor with IC50 of 0.625 μM and 16 μM in RCC4 and RCC4 VHL cells, respectively.

Zifcasiran, a hypoxia-inducible factor (HIF) synthesis reducer, exhibits antitumor activities and is utilized in advanced renal cell carcinoma research [1] [2].

Elsilimomab (B-E8) is a monoclonal antibody targeting interleukin-6 (IL-6), inhibiting DNMT3A mutant clone-induced hematopoietic stromal cell senescence, used in the study of multiple myeloma and renal cell carcinoma.

Sonepcizumab (LT 1009) is a fully humanized monoclonal antibody against S1P, with anti-cancer activity, useful for studying metastatic renal cell carcinoma (mRCC) and preventing eye scarring after glaucoma filtration surgery.

XPW1 is a new potent and selective CDK9 inhibitor with antitumour activity that transcriptionally inhibits the DNA repair process in ccRCC cells.XPW1 can be used to study clear cell renal cell carcinoma.

Naptumomab, a tumor-targeting superantigen (TTS), is a fusion protein that activates the immune system to recognize and eradicate tumor cells. It shows promise in researching refractory solid tumors, including renal cell carcinoma [1] [2].