oncology

EPZ020411 is a specific and effective inhibitor of PRMT6 (IC50=10 nM).

The Immuno-Oncology Screening Library consists of 2 plates and contains more than 90 cancer and immunology-associated compounds in a 96-well Matrix tube rack format as 10 mM stock solutions in DMSO. This library includes a variety of immuno-oncology target modulators, including but not limited to, adenosine, CCR, CXCR, and TLR agonists and antagonists, BTK, PI3K, VEGFR, and BRAF inhibitors, PD-1/PDL-1 interaction inhibitors, and HDAC inhibitors. Please review the product insert for a full list of targets. Stability data is not available for the compounds as supplied in the screening library.

GSK864 is an IDH1 mutant inhibitor that inhibits IDH1 mutants R132C, R132H, and R132G, and is used in the study of cardiovascular and oncology diseases.

ART558 is a potent, selective, low molecular weight, allosteric DNA polymerase activity of Polθ inhibitor (IC50=7.9 nM). ART558 can be used for the research of cancer.

Izonsteride (LY320236) is a selective and potent 5alpha reductase inhibitor with dual action on the type I and type II isoforms of the enzyme.Izonsteride is used in the treatment of oncology and genitourinary disorders, and may be used in the study of prostate cancer.

Numidargistat dihydrochloride (CB-1158 dihydrochloride) is an orally active and highly effective arginase (ARG1) inhibitor, an immuno-oncology agent that inhibits TGF-β2-induced subcapsular cataract by reducing the proliferation of lens epithelial cells (LEC) and decreasing the expression of fibronectin, α-SMA, collagen 1A1, and vimentin.

GSK040, a potent and highly selective inhibitor of BET BD2, exhibits a pIC50 of 8.3, demonstrating over 5000-fold selectivity against BET BD1 (pIC50=4.6). This compound is primarily utilized in oncology and immunology research [1].This compound is unstable in powder form and other related salt forms are recommended.

Floxuridine (FUDR) is an antimetabolite, floxuridine inhibits thymidylate synthase, resulting in disruption of DNA synthesis and cytotoxicity.

GDC-2992 is a selective and oral AR (androgen receptor) degrader that inhibits the proliferation of tumor cells overexpressing AR, degrades AR (DC50 = 2.7 nM) and inhibits proliferation (IC50 = 9.7 nM) in VCaP cells, and can be used for oncology studies in denuded resistant prostate cancer (CRPC).

CZ415 is a potent and highly selective mTOR inhibitor. This compound has a molecular weight of 432.51 g mol and demonstrates an inhibition constant (IC50) of 5.8 nM against mTOR. Additionally, CZ415 has shown to be efficacious in preclinical models of cancer, indicating its potential therapeutic application in oncology.

Compound 4a, also known as hA2AAR antagonist 1, is a highly selective hA2AAR antagonist with a Ki value of 5 nM. It is useful in the field of immuno-oncology research.

GSK217 is a potent and selective inhibitor of the bromo and extraterminal domain (BET) second bromodomain (BD2) with high solubility, utilized in oncology and immune inflammation research [1].

Interleukin-6 Fragment (human) is a pleiotropic cytokine originating from both lymphocytes and non-lymphocytes, encoded by a gene on human chromosome 7 spanning roughly 5 kilobases. This fragment shows promise for use in immune response regulation, acute phase reactions, inflammatory processes, oncology, and hematopoiesis [1].

Crotalicidin, obtained from rattlesnake venom, is both an antimicrobial and anti-tumor peptide with potent efficacy against Gram-negative bacteria and cancerous cells, showing promise for research in microbial infections and oncology [1].

UK-356,202 is a potent and selective urokinase-type plasminogen activator (Ki = 37 nM). Urokinase plasminogen activator (uPA, urokinase) is a trypsinlike serine protease and a therapeutical target for many cancer types, including breast, ovarian, and pancreatic cancer. uPA is a valuable oncology target.

Tarlatamab (AMG-757) is a first-in-class, high-affinity bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3), a protein primarily expressed in small-cell lung cancer (SCLC) with minimal expression in normal tissues. It has dissociation constants (KDs) of 0.64 nM and 0.50 nM for DLL3 in human and nonhuman primates (NHP), respectively, and 14.9 nM and 12 nM for CD3 in human and NHP, accordingly. As a pioneering HLE BiTE immuno-oncology therapy for DLL3-expression SCLC, tarlatamab shows promising potential for research in this area [1].

6-Aminocaproic acid-(S,R,S)-AHPC-Me serves as a ligand and linker for the E3 ubiquitin ligase in PROTACs, facilitating the synthesis of PVD-06 for research in oncology.

iBRD4-BD1 diTFA is a selective BRD4 bromodomain inhibitor with an IC50 value of 12 nM. It can be used for research in inflammation and oncology [1].

Inupadenant is an orally active, highly selective A2A receptor antagonist with potent anti-tumor activity [1] and is not brain-penetrant.

1,2-Dilinoleoyl-sn-glycero-3-phospho-L-serine sodium is a lipid compound utilized in the formulation of liposomes. Liposomes, composed of concentric phospholipid bilayer vesicles, serve as integral components in drug delivery systems aimed at oncology and anti-infection treatments. They efficiently encapsulate hydrophilic (highly polar) solutes within their aqueous interior, while lipophilic solutes are integrated into and become part of the lipid bilayer. This compound is particularly effective in delivering antisense oligonucleotides, addressing challenges such as poor cellular uptake and rapid degradation in the body.

iBRD4-BD1 is a selective inhibitor of the BRD4 bromodomain, exhibiting inhibition activity with an IC50 value of 12 nM. It is utilized in the research of inflammation and oncology.

I-BET567, a potent pan-BET inhibitor with oral activity, demonstrates pIC50 values of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. This compound has exhibited efficacy in mouse models of oncology and inflammation [1].

TGFβRI-IN-3 is a highly selective TGFβR1 inhibitor with an IC50 of 0.79 nM and exhibits 2000-fold selectivity against MAP4K4, showing potential applications in immuno-oncology [1].

Mutant IDH1-IN-3 (Compound 1) is a selective allosteric inhibitor targeting the mutant isocitrate dehydrogenase 1 (IDH1), with an IC50 of 13 nM for R132HIDH1. It effectively suppresses the production of D-2-hydroxyglutarate (2HG) in cells and is applicable for research in oncology.