Antitumoragent-28 is a compound that specifically targets and inhibits the activity of the ataxia telangiectasia mutated (ATM) kinase. By doing so, it effectively impedes the progression of ATM-mediated diseases and demonstrates significant anti-cancer activity.
Antitumoragent-23 exhibits potent antitumoral activity, as demonstrated by its GI50 values of 38, 48, 5, 27, 80, and 28 nM against the lymphoma cell lines GRANTA-519, KARPAS-422, KARPAS-299, RAMOS, DAUDI, and RAJI respectively.
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces and a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM, it also is an apoptosis inducer. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase, it also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin has antiproliferative and antitumor activities[1][2][3][4][5].
CB 300919 is a quinazoline-based antitumoragent with high activity in the CH1 human ovarian tumor xenograft and has continuous exposure (96 h) growth inhibition (IC50: 2 nM).
Duocarmycin A, an antitumor antibiotic, is a DNA alkylator and efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results in HLC-2 cells typically apoptotic changes.
Physapubenolide is natural cytotoxic withanolide antitumoragent. Physapubenolide induces apoptosis by decreasing mitochondrial membrane potential and elevating the Bax Bcl-2 protein expression ratio.
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 antitumoragent 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)
cDPCP is a platinum-containing DNA-crosslinking agent.1Unlike cisplatin or oxaliplatin , cDPCP forms monofunctional DNA adducts. It is transported into cells by organic cation transporter 1 (OCT1) and OCT2, inhibiting proliferation of MDCK cells expressing the human transporters with IC50values of 8.1 and 1.5 μM, respectively. cDPCP inhibits RNA polymerase II-mediated transcription in a reporter assay using HeLa cells. It increases survival in murine S180 sarcoma and P388 leukemia models when administered at doses of 40 and 80 mg/kg, respectively.2 1.Lovejoy, K.S., Todd, R.C., Zhang, S., et al.cis-Diammine(pyridine)chloroplatinum(II), a monofunctional platinum(II) antitumoragent: Uptake, structure, function, and prospectsProc. Natl. Acad. Sci. USA105(26)8902-9807(2008) 2.Hollis, L.S., Amundsen, A.R., and Stern, E.W.Chemical and biological properties of a new series of cis-diammineplatinum(II) antitumoragents containing three nitrogen donors: cis-[Pt(NH3)2(N-donor)Cl]+J. Med. Chem.32128-136(1989)
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].