renal cell carcinoma

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.

Nivolumab is a monoclonal antibody and is a humanized PD-1 antibody. Nivolumab has anti-tumor activity and is used in the treatment of melanoma, non-small cell lung cancer, renal cell carcinoma, etc.

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, PT2977) is a small-molecule inhibitor and a HIF-2α inhibitor (IC50 = 9 nM) with high selectivity, oral activity, and improved pharmacokinetic characteristics, used for the treatment of clear cell renal cell carcinoma and related VHL diseases.

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

Histamine (Ergamine) is an amine derived from histamine through enzymatic decarboxylation; it acts as a histamine receptor agonist and vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses and regulates intestinal physiological functions. Histamine is a potent stimulant of gastric secretion, a bronchoconstrictor, a vasodilator, and a centrally acting neurotransmitter. Histamine influences the p38 MAPK/Akt signaling pathway and exhibits antitumor, antioxidant, and anti-inflammatory activities. Histamine can be used in research on acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.

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

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.

JNK-1-IN-3 (Compound 9e) is a JNK1 inhibitor that downregulates JNK1 and phosphorylated JNK1, reduces c-Jun and c-Fos expression in tumours, and restores p53 activity. JNK-1-IN-3 exhibits potent antiproliferative activity against renal carcinoma and breast cancer cell lines.

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.

Z57346765 hydrochloride is an inhibitor of phosphoglycerate kinase 1 (PGK1) that binds to the ADP binding site, with a K\(_D\) value of 2.09 × 10⁻⁵ M, thereby reducing the metabolic enzyme activity of PGK1, glucose consumption, and lactate production. Additionally, it inhibits DNA replication, impairs DNA damage repair, and induces cell cycle arrest in renal clear cell carcinoma (KIRC) cells.

SPOP-IN-2 (Compound E1) is a potent inhibitor of speckle-type POZ protein (SPOP), with an IC50 of 0.58 μM. It disrupts the interaction between SPOP and substrates and selectively inhibits the proliferation of clear cell renal cell carcinoma (ccRCC).

CAIX-IN-4 (Compound 8b) is a selective inhibitor of carbonic anhydrase IX (CAIX) with an IC50 value of 0.32 μM. It holds potential for research in cancer, such as renal cell carcinoma.

PWT-33597 (VDC-597) free base is a dual inhibitor of PI3Kα and mTOR that effectively obstructs downstream signaling pathways of PI3K and mTOR. This compound induces apoptosis in tumor cells and inhibits tumor growth. PWT-33597 free base demonstrates antitumor activity and can be used in research related to renal cell carcinoma and other tumors.

DDO-4033 is an SPOP inhibitor with an IC50 of 16.9 μM and a Kd of 15.1 μM. It hinders the malignant migration, invasion, and proliferation of clear cell renal cell carcinoma (ccRCC) cell lines. DDO-4033 disrupts the recruitment of the substrate LATS1 by SPOP, inhibiting its polyubiquitination and subsequent degradation, which leads to the upregulation of LATS1 expression. This compound demonstrates significant antitumor activity and can be utilized in renal cell carcinoma research.

GPX4-IN-18 (Compound 17) is a ferrocene-containing inhibitor of glutathione peroxidase 4 (GPX4), and it also acts as a ferroptosis inducer. It enhances the production of reactive oxygen species (ROS) and malondialdehyde (MDA) levels in OS-RC-2 clear cell renal carcinoma cells. In HT-1080 cells, GPX4-IN-18 induces ferroptosis with IC50 values of 0.007 μM (without iron inhibitor-1) and 1.486 μM (with iron inhibitor-1). Additionally, GPX4-IN-18 reduces tumor volume and intratumoral GPX4 levels in an OS-RC-2 xenograft mouse model.

Sunitinib-platinum(IV) prodrug-1 (Complex A) is a Cisplatin-based Pt(IV) prodrug designed to be reduced to active Pt(II) in intracellular reductive conditions, while concurrently releasing a sunitinib derivative with tyrosine kinase inhibitor (TKI) activity. This compound exhibits remarkable cytotoxicity against renal cell carcinoma (RCC), inducing DNA crosslinking and apoptosis. It inhibits VEGFR/PDGFR signaling pathways, thereby suppressing tumor growth and angiogenesis, and can be used for studying RCC.

NEO-811 is a potent, selective, and cereblon (CRBN)-dependent E3 ubiquitin ligase-mediated proteolytic inhibitor that targets ARNT (HIF-1β). NEO-811 blocks ccRCC signaling pathways by promoting degradation of ARNT, thereby inhibiting tumor cell survival and proliferation. NEO-811 is used in targeted protein degradation research systems to study CRBN-dependent ubiquitination, hypoxia-inducible factor signaling regulation, and clear cell renal cell carcinoma (ccRCC) molecular pathway modulation in cellular oncology models.

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