antitumor agent 4

Antitumor agent-4 is a butenylphenyl phosphate derivative, is an agent of mammary cancer and anovulatory sterility.

4-(Benzo[d]oxazol-2-yl)aniline is a potent antitumor agent with inhibitory activity against mammary carcinoma cell lines [1].

Fulvene-5 is a chemical compound that exhibits antitumor activity. It functions as a potent inhibitor of NADPH oxidase 4 (NOX4) and possesses antioxidant properties. Additionally, Fulvene-5 acts as a reactive oxygen species (ROS) modifying agent and a powerful radioprotector.

Actinonin is a natural antibacterial agent produced by Streptomyces, also serving as an effective PDF (peptide deformylase) inhibitor and apoptosis inducer. It inhibits APN (Aminopeptidase N), MMPs and heparin α, exhibiting antiproliferative and antitumour activity.

Desacetylvinblastine (4-Desacetylvinblastine) is a primary metabolite of vinblastine and functions as a cytotoxic agent. While its antitumor efficacy is limited when used alone, it can exhibit significant antitumor activity when involved as part of specific conjugates.

Antitumor agent-198 (Compound A3) exhibits cytotoxicity in head and neck squamous cell carcinoma (HNSCC) cells, effectively inhibiting the proliferation of CAL27, HN6, HN30, SCC9, and SCC25, with an IC50 ranging from 4 nM to 77 nM. Additionally, Antitumor agent-198 suppresses HNSCC cell migration, arrests the cell cycle, and induces apoptosis.

4'-epi-Daunorubicin is the semisynthetic precursor to Epirubicin and functions as an antitumor agent.

Antitumor agent-129 (Compound 68) is a derivative of thiazolidine-4-thione and an inhibitor of osteosarcoma (OS), with an IC50 value of 0.217 μM against OS cell activity. It has a half-life of 73.8 minutes in mouse liver microsomes and exhibits favorable pharmacokinetic properties with an in vivo bioavailability (F) of 115% following intraperitoneal administration. Antitumor agent-129 is a potential candidate for OS research.

KRN7000 analog 1 stimulates a strong Th1-biased immune response by inducing interferon-γ (IFN-γ) and reducing interleukin-4 (IL-4). This compound shows potential as an antitumor agent and vaccine adjuvant.

DMPEN (NSC 682691) (4-Demethylpenclomedine) is a metabolite of the alkylating agent Penclomedine. It exhibits antitumor activity and does not induce Purkinje cell loss or significant cerebellar neurotoxicity in rat cerebellum models. DMPEN is applicable in cancer research, including studies on breast and brain cancer.

4-oxo Cyclophosphamide is an inactive metabolite of the alkylating agent cyclophosphamide .1,2It is formed from cyclophosphamide through a 4-hydroxycyclophosphamide intermediate by aldehyde dehydrogenases.2 1.Struck, R.F., Kirk, M.C., Mellett, L.B., et al.Urinary metabolites of the antitumor agent cyclophosphamideMol. Pharmacol.7(5)519-529(1971) 2.de Jonge, M.E., Huitema, A.D.R., Rodenhuis, S., et al.Clinical pharmacokinetics of cyclophosphamideClin. Pharmacokinet.44(11)1135-1164(2005)

LSN3106729 hydrochloride, the metabolite of Abemaciclib , is a CDK inhibitor with antitumor activity. LSN3106729 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1]. [1]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non-Small Cell Lung Cancer: A Phase Ib Study. [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use. WO2017185031A1.

Loxoprofen sodium dihydrate is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. It exhibits antitumor activity and can reduce atherosclerosis. This compound is a nonselective inhibitor of COX with IC50 values of 6.5 μM for COX-1 and 13.5 μM for COX-2 [1] [2] [3] [4].

Antitumor agent-66 (Compound 4) is a derivative of (-)-cleistenolide, exhibiting potential as a research tool for cancer diseases [1].

Antitumor agent-77 inhibits the growth and migration of cancer cells and has anticancer effects. antitumor agent-77 inhibits GPx-4 and enhances COX2-induced iron sagging. antitumor agent-77 activates the intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) in tumor cells and prevents tumor cell epithelialization. Antitumor agent-77 activates the tumour cell intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and blocks the epithelial mesenchymal transition (EMT) process.

Antitumor agent-78 inhibits GPx-4 and elevates COX2, leading to ferroptosis. antitumor agent-78 activates the tumor cell intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and inhibits the epithelial mesenchymal transition (EMT) process in tumor cells. Antitumor agent-78 exhibits antitumor effects and inhibits the growth and migration of cancer cells.

STA-9584 is a potent vascular disrupting agent, which exhibits potent antitumor activity by selectively targeting microvasculature at both the center and periphery of tumors. In vitro, 2-methoxy-5-(5-(3,4,5-trimethoxyphenyl)isoxazol-4-yl)aniline (STA-9122) (active metabolite of STA-9584 ) displayed increased potency relative to other tubulin-binding agents and was highly cytotoxic to tumor cells. STA-9584 induced significant tumor regressions in prostate and breast xenograft models in vivo and, in an aggressive syngeneic model, demonstrated superior tumor growth inhibition and a positive therapeutic index relative to combretastatin A-4 phosphate (CA4P).

APTO-253, also known as LOR-253, LT-253, is a small molecule inhibitor of human metal-regulatory transcription factor 1 (MTF-1) with potential antitumor activity. MTF-1 inhibitor LOR-253 inhibits MTF-1 activity and thereby induces the expression of MTF-1 dependent tumor suppressor factor Kruppel like factor 4 (KLF4). This subsequently leads to the downregulation of cyclin D1, blocking cell cycle progression and proliferation. This agent also causes decreased expression of genes involved in tumor hypoxia and angiogenesis.

APTO-253 isomer is an isomer of APTO-253 with the Fluoro-atom in 6-position. APTO-253 also known as LOR-253, LT-253, is a small molecule inhibitor of human metal-regulatory transcription factor 1 (MTF-1) with potential antitumor activity. MTF-1 inhibitor LOR-253 inhibits MTF-1 activity and thereby induces the expression of MTF-1 dependent tumor suppressor factor Kruppel like factor 4 (KLF4). This subsequently leads to the downregulation of cyclin D1, blocking cell cycle progression and proliferation. This agent also causes decreased expression of genes involved in tumor hypoxia and angiogenesis.