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.

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.

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.

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.

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.

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.

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.

KRAS inhibitor-10 (WO2021005165 A1, compound 11) is a potent and selective inhibitor of RAS proteins, with a specific focus on KRAS proteins. This orally active anti-cancer agent demonstrates strong efficacy in cancer research, specifically in pancreatic cancer, breast cancer, multiple myeloma, leukemia, and lung cancer. KRAS inhibitor-10 is classified as a tetrahydroisoquinoline compound. Its inhibitory properties provide valuable insights and potential therapeutic applications in the field of oncology [1].

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

3-hydroxy-3-phenylpentanamide is a chiral compound belonging to the class of beta-hydroxyamides. In neurology, it has been shown to have neuroprotective effects against ischemic brain injury and cerebral hemorrhage. In psychiatry, it has been studied as a potential treatment for anxiety, depression and addiction. In oncology, it has been shown to have antitumor activity by inducing apoptosis and inhibiting tumor growth.

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.

AC430 is a potent and specific small molecule inhibitor of janus kinase 2 (JAK2), which has been implicated as a target for therapy in both oncology and autoimmune disease. AC430 is currently being developed by Ambit. In preclinical studies, AC430 has exhibited potency against JAK2 and V617F mutated JAK2 in cell-based models that is at least equivalent to, and in most cases superior to, competing JAK2 inhibitors. In preclinical oncology and autoimmune models, AC430 is well tolerated and has significant efficacy at oral doses as low as 10 mg kg day.