oncology

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

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.

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.

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.

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.

ACLY Inhibitor 7 is a highly potent and selective small molecule inhibitor that exhibits exceptional inhibitory activity against human ATP citrate lyase (hACLY). ACLY Inhibitor 7 demonstrates an IC50 value of less than 1 nM as measured by the ADP-Glo assay, indicating its potential for metabolic disease and oncology research.

GDC-2992 is a selective and orally active androgen receptor (AR) degradator that degrades AR (DC50 = 2.7 nM) and inhibits proliferation (IC50 = 9.7 nM) in VCaP cells, making it suitable for studying castration-resistant prostate cancer (CRPC).

CG347B is a selective inhibitor of HDAC6.

PARP1-IN-29 is an orally active PARP-1 inhibitor with an IC50 of 6.3 nM. When labeled with [18F], PARP1-IN-29 can be utilized for positron emission tomography (PET) imaging, specifically targeting PARP-1 in tumors. This compound is useful in oncology and imaging studies, particularly for detecting PARP-1 activity in cancer.

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.

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.

Gintemetostat (KTX-1001) is a potent and selective small molecule inhibitor of nuclear receptor-binding SET domain protein 2 (NSD2), exhibiting IC50 values ranging from 0.001 μM to 0.01 μM, and it belongs to the chemical class of piperidinyl-methyl-purineamine derivatives, with primary research applications in oncology for the treatment of NSD2-dysregulated cancers.

USP7-IN-16 (Compound 61) is a selective inhibitor of USP7, with IC50 values of 5.5 nM in the FLINT assay and 2.1 nM in MM.1S cells. This compound exhibits antitumor activity in mice and holds potential for research in the field of oncology.

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.

IIP0943 is a selective PLK1 (polo-like kinase 1) inhibitor with an IC50 of 5.1 nM for PLK1. It also exhibits inhibitory activity on the proliferation of HCT116 cells, with an IC50 of 0.22 µM. IIP0943 shows potential for research in the field of oncology.

HIF-PHD-IN-4 (Compound 13) is an orally active PHD2 inhibitor with an IC50 of 100 nM. At a dose of 2 mg/kg, it effectively enhances G-CSF-induced mobilization of hematopoietic stem cells in mice. HIF-PHD-IN-4 is suitable for research in the oncology field.

LEQ803 (N-DesmethylRibociclib) is a metabolite of the CDK4/6 inhibitor Ribociclib, produced through metabolism by CYP3A4. This compound holds potential applications in the field of oncology.

Mavelertinib (PF-06747775) is an orally available, selective and potent EGFR tyrosine kinase (EGFR TKI) inhibitor with inhibitory effects on T790M/L858R and T790M/Del, and can be used in the study of oncology and respiratory diseases.

AZD8542 is an antagonist of Smoothened (SMO) with potential as an [oncology therapeutic].

Fluoroethyl-l-tyrosine (18F) or 18F-FET is a neuro-oncology PET tracer.

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.