adenocarcinoma

CAN508 is a potent ATP-competitive CDK9 cyclin T1 inhibitor with an IC50 of 0.35 μM. It also competitively inhibits Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 μM and 20 μM, respectively. CAN508 exhibits a 38-fold selectivity for CDK9 cyclin T over other CDK cyclin complexes. [Antitumor activity.]

Ellipticine (Elliptisine) is a potent antineoplastic agent exhibiting multiple mechanisms of action, IC50 of 0.67±0.06, 1.25±0.13, 1.25±0.13, 0.67±0.06, 0.27±0.02, 0.49±0.04, 0.44±0.03, and 1.48±0.62 μM for Leukemia HL-60, Breast adenocarcinoma MCF-7, Breast adenocarcinoma MCF-7, Leukemia HL-60, Neuroblastoma IMR-32, Neuroblastoma UKF-NB-4, Neuroblastoma UKF-NB-3, and Glioblastoma U87 mg cell, respectively.

Tegadifur (40497S) is an orally available antitumor compound with antimetabolic effects, often used with uracil and in the treatment of rectal adenocarcinoma.

Vinaxanthone (SM-345431) is a small molecule compound derived from Penicillium chrysogenum that acts as a selective and potent inhibitor of semaphorin3A, phospholipase C (PLC), and FabI, exhibiting antimicrobial activity by blocking intracellular fatty acid synthesis and inhibiting the growth of Staphylococcus aureus.

Bexlosteride (LY300502), a benzoquinolinone derivative, functions as a human type I 5α-reductase inhibitor. It demonstrates metabolic inhibition, antiproliferative, and antisecretory activities specifically in LNCaP human prostatic adenocarcinoma cell cultures, positioning it as a potent agent for prostate cancer research [1] [2].

Silibinin (Silybin) is the major active constituent of silymarin, a standardized extract of the milk thistle seeds, containing a mixture of flavonolignans consisting of silibinin, isosilibinin, silicristin, silidianin and others. Silibinin itself is a mixture of two diastereomers, silybin A and silybin B, in approximately equimolar ratio. Both in vitro and animal research suggest that silibinin has hepatoprotective (antihepatotoxic) properties that protect liver cells against toxins. Silibinin has also demonstrated in vitro anti-cancer effects against human prostate adenocarcinoma cells, estrogen-dependent and -independent human breast carcinoma cells, human ectocervical carcinoma cells, human colon cancer cells, and both small and nonsmall human lung carcinoma cells.

6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile is a PDK1 inhibitor with anticancer and antiproliferative activity that can be used to study angiosarcoma, adenocarcinoma, multiple myeloma, psoriasis, prostate cancer, and Alzheimer's disease.

KY-05009 is a chemical compound that effectively suppresses TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells, reduces TNIK protein expression and the transcriptional activity of Wnt target genes, and promotes apoptosis in cancer cells, displaying anti-cancer properties. Furthermore, it functions as an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM.

SMIFH2 is formin homology 2 (FH2) domains inhibitor.

Rosmanol has antioxidant activity, it can activate the antioxidant response element. Rosmanol has biphasic modulation of GABAA receptors, demonstrates CNS activity in mouse models of antinociception, antidepressant and anxiolysis. Rosmanol potently induce

Brigimadlin (BI 907828) is an orally active and highly potent E3 ubiquitin-protein ligase MDM2-p53 antagonist with antitumor activity.Brigimadlin can be used to study metastatic BTC, PDAC, lung adenocarcinoma, or bladder cancer.

PARP-1-IN-2 is a potent PARP1 inhibitor that crosses the blood-brain barrier (IC50: 149 nM).PARP-1-IN-2 showed significant antiproliferative activity against the human lung adenocarcinoma epithelial cell line A549 in cellular assays.PARP-1-IN-2 induced apoptosis in A549 cells.

BCAT-IN-4 is a potent BCAT inhibitor with an IC50 value of 2.35 μM for hBCATc. BCAT-IN-4 has anticancer activity and can be used to study pancreatic ductal adenocarcinoma.

BPI-9016M is an effective, orally active, and selective dual inhibitor of c-Met and AXL tyrosine kinases. It suppresses tumor cell growth, invasion, and migration of lung adenocarcinoma.

SBI-797812 is structurally similar to active-site directed inhibitor of NAMPT(NAMPT with EC50 of 0.37 μM).

GSK319347A is a selective and potent dual inhibitor of TBK1 and IKKε with potential anti-tumor activity and inhibition of IKK2 activity, which can be used in the study of bladder cancer and lung adenocarcinoma.

Chemically modified tetracyclines (CMTs) can inhibit MMPs, but lack antimicrobial activity. Nonantimicrobial derivative of tetracycline called incyclinide (COL-3, CMT-3). Incyclinide (CMT-3) has been shown to experimentally suppress prostate cancer, colon adenocarcinoma and melanoma invasiveness in cell culture and to inhibit tumor growth and metastasis.

PARP1-IN-31 (compound 11f), a thiazolopyridone-based compound, exhibits potent inhibition against PARP-1, with an IC50 value of 97 nM. It acts as an anti-lung adenocarcinoma agent, capable of inducing apoptosis and inhibiting cell proliferation in lung cancer cell lines.

4'-Hydroxytamoxifen TFA, a salt form of a metabolite of Tamoxifen, demonstrates higher affinity for ER compared to Tamoxifen itself. This compound induces non-apoptotic cytotoxicity in human endometrial adenocarcinoma cells.

DSPE-PEG(2000) maleimide is a PEGylated derivative of 1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE). This compound is frequently utilized both in vitro and in vivo for synthesizing lipid nanoparticles (LNPs) that deliver siRNA or small molecule anticancer drugs. In experiments, LNPs containing DSPE-PEG(2000) maleimide and encapsulating siRNA targeting the mRNAs for p53 and K-RAS induced tumor regression in a PANC-1 pancreatic ductal adenocarcinoma mouse xenograft model.

68Ga-DOTA-NT-20.3 is an analogue of neurotensin (NTS) and acts as a ligand for 68Ga ions. In PET imaging, it demonstrates rapid tumor uptake and high contrast between tumor and background, along with fast clearance from the blood and moderate accumulation in the kidneys. Its pharmacokinetic and biodistribution properties are advantageous, producing high-quality PET images in mice with subcutaneous or orthotopic human pancreatic cancer xenografts. 68Ga-DOTA-NT-20.3 specifically binds to NTSR1 on pancreatic cancer cells and outperforms 18F-FDG in PET detection of adenocarcinoma.

Azaspirene, a novel angiogenesis inhibitor, is based on the 1-oxa-7-azaspiro[4.4]non-2-ene-4,6-dione framework. Previous studies have shown that Azaspirene effectively inhibits VEGF-induced migration of human umbilical vein endothelial cells (HUVEC), demonstrating a potentially effective dosage. Moreover, azaspirene analogs may exhibit potential antitumor effects against uterine adenocarcinoma, possibly through significant anti-angiogenic activity.

UNBS3157 is a novel naphthalimide derivative that is non-hematotoxic and exhibits significant antitumor activity through DNA intercalation and the poisoning of topoisomerase IIalpha. Unlike Amonafide, a related naphthalimide compound that showed activity in Phase II breast cancer trials but did not proceed to Phase III due to dose-limiting myelotoxicity, UNBS3157 has a maximum tolerated dose 3-4 times higher and does not cause hematotoxicity in mice at effective antitumor doses. In vivo models, including (i) L1210 mouse leukemia, (ii) MXT-HI mouse mammary adenocarcinoma, and (iii) human A549 non-small cell lung carcinoma and BxPC3 pancreatic cancer orthotopic models, demonstrate superior efficacy of UNBS3157 compared to Amonafide.

SBI-183 is an orally active QSOX1 inhibitor (Kd: 20 μM). It can inhibit the proliferation and invasion phenotypes of renal carcinoma cell lines, triple-negative breast cancer cell lines, lung adenocarcinoma cell lines, and pancreatic ductal adenocarcinoma. In vivo, SBI-183 suppresses tumor growth in two human renal cell carcinoma xenograft mouse models.