adrenocortical carcinoma

Mitotane (NCI-C04933) is a derivative of the insecticide DICHLORODIPHENYLDICHLOROETHANE that specifically inhibits cells of the adrenal cortex and their production of hormones. It is used to treat adrenocortical tumors and causes CNS damage, but no bone marrow depression.

Perthane is the diethyl derivative of common pesticide DDD. It may cause adrenocortical atrophy in humans,and also prevent the formation of spontaneous mammary carcinoma.

Tetrahydro-11-deoxy cortisol (THS) is the primary urinary metabolite of 11-deoxycortisol. Urinary excretion of THS is elevated in patients with 11β-hydroxylase deficiency, a condition resulting from mutations in the cytochrome P450 (CYP) isoform CYP11B1. Urinary levels of THS are also elevated in patients with adrenocortical carcinoma (ACC) and adrenocortical adenoma (ACA) but are higher in patients with ACC compared to ACA.

SID7970631 is an isoquinolinone analog and a potent, selective submicromolar SF-1 (Steroidogenic Factor-1, NR5A1) inhibitor/inverse agonist with an IC50 of 255 nM. It inhibits SF-1-mediated transcriptional activity and exhibits significant cytotoxic effects on SF-1-dependent cancer cell lines. SID7970631 is widely utilized in research exploring therapeutic mechanisms for cancers such as adrenocortical carcinoma.

Efonidipine HCl (NZ-105) serves as both a T-type and L-type calcium channel blocker. This compound, distinct from other calcium channel blockers, notably increases N(6), 2'-O-dibutyryladenosine 3',5'-cyclic monophosphate (dbcAMP)-induced StAR mRNA and DHEA-S production in NCI-H295R adrenocortical carcinoma cells, actions reflective of adrenocorticotropic hormone. Efonidipine uniquely inhibits calcium channels by merging tonic and use-dependent blocking methods. Its inhibitory concentrations (IC50) for I(Ca(T)) and I(Ca(L)) are 0.35 micromol/l and 1.8 nmol/l, respectively. Clinically, efonidipine administered to hypertensive patients undergoing chronic hemodialysis (20-60 mg, twice daily) demonstrated comparable blood pressure control to amlodipine (2.5-7.5 mg, once daily) over a 12-week period without significantly altering pulse rate. Furthermore, efonidipine significantly improved left ventricular ejection fraction in heart failure models without affecting blood pressure, in addition to lowering the heart rate by about 10%.

FHD-609 is an effective BRD9 inhibitor and PROTAC degrader, targeting the non-classical BAF (ncBAF) subunit BRD9, thereby depleting the SS18-SSX fusion protein, and can be used for the study of synovial sarcoma (SS).

Efonidipine hydrochloride monoethanolate (NZ-105 hydrochloride monoethanolate) is a Ca(2+)-channel blocker that enhances the production of dehydroepiandrosterone sulfate in NCI-H295R human adrenocortical carcinoma cells.

CBP-1008 is a dual-ligand peptide-drug conjugate (PDC) with MMAE, targeting folate receptor (FRα) and TRPV6. It exhibits high binding affinity to FRα and low affinity to TRPV6. CBP-1008 shows antitumor activity and can be utilized for research in advanced solid tumors such as colorectal cancer, breast cancer, non-small cell lung cancer, ovarian cancer, adrenocortical carcinoma, and follicular dendritic cell sarcoma.