anti tumor

AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1.

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

AZD-7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK) with the IC50 of 0.63 nM in an enzyme assay,has anti-tumor activity.

Adagrasib (MRTX849) is an orally active and selective covalent inhibitor of KRAS G12C. Adagrasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Adagrasib exhibits inhibitory activity against KRAS G12C mutant tumors.

MSAB is a selective inhibitor of Wnt/β-catenin signaling. MSAB binds to β-catenin, promoting its degradation, and specifically downregulates Wnt/β-catenin target genes.

Panitumumab is a fully human IgG2 monoclonal antibody targeting the epidermal growth factor receptor EGFR).

BMS-202 (PD1-PDL1 inhibitor 2) is an inhibitor of the PD-1 (Programmed death- 1) /PD-Ll (Programmed death-ligand 1) protein/protein interaction.

GSK1904529A (GSK 4529) is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .

Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an aromatic diamidine agent effective against various microorganisms, including protozoa (Trypanosoma brucei, Leishmania spp., and Babesia spp.) and fungi (Pneumocystis jirovecii). It is a potent and selective inhibitor of protein tyrosine phosphatases and phosphatase of regenerating liver. Pentamidine dihydrochloride inhibits the parasite Leishmania infantum with an IC50 of 2.5 μM.

AKB-6899 is an inhibitor of prolyl hydroxylase domain 3 (PHD3) and increases the soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages. AKB-6899 leads to stabilization of HIF-2α which induces sVEGFR-1 production from tumor-associated macrophages and decreases tumor growth.

ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2/3/4. It is used in the research on inflammatory diseases, cancer, and AIDS.

Tubulin inhibitor 24 is a potent compound that inhibits tubulin polymerization.

K145 hydrochloride is a selective sphk2 inhibitor with substrate competitiveness and oral activity, with IC50 of 4.3 µM and Ki of 6.4 µM. K145 hydrochloride can induce apoptosis and has strong antitumor activity.

Ibuprofen (Advil) is a propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. Ibuprofen inhibits the activity of cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes.

Dorzolamide hydrochloride (MK507 hydrochloride) is the hydrochloride salt form of dorzolamide, an inhibitor of carbonic anhydrase, a zinc-containing enzyme that catalyzes the rapid conversion of carbon dioxide and water into carbonic acid, protons and bicarbonate ions. Distributed throughout many cells and tissues, various carbonic anhydrases play important roles in mineral and metabolic homeostasis.

Niraparib (MK-4827) is a PARP inhibitor that selectively targets PARP1 and PARP2 (IC50=3.8/2.1 nM), exhibiting antitumor activity, inhibiting DNA damage repair, and inducing apoptosis.

Dipyrithione appears to have novel cytotoxicity and potent broad-spectrum antitumor activity

Niraparib, also know as MK-4827, is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway.

Mitoxantrone dihydrochloride (NSC-301739) is the hydrochloride salt of an anthracenedione antibiotic with antineoplastic activity. It is a type II topoisomerase inhibitor.

Erythromycin (E-Mycin) is a Macrolide and Macrolide Antimicrobial. The physiologic effect of erythromycin is by means of Decreased Sebaceous Gland Activity.

Hesperidin (Cirantin) is a flavanone glycoside found in citrus fruits with antioxidant, anti-inflammatory, anti-carcinogenic, and antihypertensive and lipid-lowering activity.

Phenoxybenzamine hydrochloride (NCI-c01661) is the hydrochloride salt form of phenoxybenzamine, a synthetic, dibenzamine alpha-adrenergic antagonist with antihypertensive and vasodilatory properties. Phenoxybenzamine non-selectively and irreversibly blocks the postsynaptic alpha-adrenergic receptor in smooth muscle, thereby preventing vasoconstriction, relieving vasospasms, and decreasing peripheral resistance. Reflex tachycardia may occur and may be enhanced by blockade of alpha-2 receptors which enhances norepinephrine release. Phenoxybenzamine is reasonably anticipated to be a human carcinogen.

Mycophenolic acid (Mycophenolate) is an inosine monophosphate dehydrogenase(IMPDH) inhibitor with anti-proliferative activity.

Dasatinib (BMS-354825) is an orally active, ATP-competitive tyrosine kinase inhibitor that targets Src and Bcr-Abl (Ki=16/30 pM), with antitumor activity, used in the treatment of leukemia and lymphoma.