chemotherapeutic agents

3PO is a small-molecule inhibitor of PFKFB3 (IC50: 22.9 μM), inhibiting the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50: 1.4-24 μM). It suppresses glucose uptake, and decreases the intracellular concentration

DODAP is an ionic cationic lipid with low cytotoxicity and high transfection efficiency that can be used to synthesize liposomes and encapsulate biologically active molecules such as mRNA, siRNA and plasmid DNA.

1. Cinnamaldehyde (Cinnamic Aldehyde) has antipyretic activity. 2. Cinnamaldehyde is a sedative agent. 3. Cinnamaldehyde inhibits invasive capabilities of MDA-MB-435S cells was correlated with down-regulating the expression of miR-27a. 4. Cinnamaldehyde induces the generation of reactive oxygen species and exerts vasodilator and anticancer effects. 5. Cinnamaldehyde appears to be a promising candidate as an adjuvant in combination therapy with 5-fluorouracil (5-FU) and oxaliplatin (OXA), two chemotherapeutic agents used in CRC treatment. The possible mechanisms of its action may involve the regulation of drugmetabolizing genes. 6. Cinnamaldehyde plays a certain role in inhibiting the occurrence and progression of melanoma and its action mechanism may be manifested by inhibiting expression of VEGF and HIF-α, thus blood vessel simulation and formation of new blood vessels of melanoma cells, and growth of tumors accordingly.

PF-477736, also known as PF-00477736, is a potent CHK1 inhibitor with potential to enhance chemotherapy. This compound inhibits CHK1, an ATP-dependent serine threonine kinase that is a crucial component of the S G2 checkpoint system for DNA replication monitoring. By bypassing the final checkpoint defenses against DNA damage-induced lethal effects, PF-477736 may improve the antitumor efficacy of various chemotherapeutic agents in tumor cells with inherent checkpoint deficiencies.

ZZ151 is an effective and selective SOS1 PROTAC with in vivo anti-tumor efficacy against KRAS-mutant cancers. This compound induces rapid and specific degradation of SOS1 and exhibits strong anti-proliferative activity against a wide range of KRAS mutation-driven cancer cells. In murine xenograft models with KRASG12D and G12V mutations, ZZ151 demonstrates superior anticancer activity. It represents a promising lead compound for developing new chemotherapeutic agents targeting KRAS mutations.

DNA-PK-IN-13 (Compound SK10) is a potent DNA-PK inhibitor, exhibiting strong inhibitory activity with an IC50 of 0.11 nM. It regulates tumor cell proliferation by reducing the expression of γH2A.X and enhancing the sensitivity of tumor cells to chemotherapeutic agents. DNA-PK-IN-13 is suitable for oncology research.

(E)-5-(2-Bromovinyl)uracil (BVU) is a pyrimidine base and an inactive metabolite of the antiviral agents sorivudine and (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU), which can be regenerated to BVDU in vivo. BVU irreversibly inactivates dihydropyrimidine dehydrogenase (DPD) in an NADPH-dependent manner, enhancing the efficacy of the chemotherapeutic agent and DPD substrate 5-fluorouracil in a P388 murine leukemia model when administered at a dose of 200 μmol kg, thereby increasing survival time.

CAY10744 is a topoisomerase II-α poison.1 It inhibits topoisomerase II-α by 78.9% when used at a concentration of 20 μM. CAY10744 is selective for topoisomerase II-α over topoisomerase I providing 100 and 0% inhibition, respectively, at 100 μM. It inhibits proliferation of HCT15 colon, T47D breast, DU145 prostate, and HeLa cervical cancer cells (IC50s = 0.014, 0.00267, 0.072, and 2.46 μM, respectively). CAY10744 induces apoptosis in T47D cells when used at concentrations of 10 and 30 μM. CAY10744 (12 mg/kg per day) reduces tumor growth in an MDA-MB-231 orthotopic mouse model of breast cancer. |1. Kadayat, T.M., Park, S., Shrestha, A., et al. Discovery and biological evaluations of halogenated 2,4-diphenyl indeno[1,2-b]pyridinol derivatives as potent topoisomerase IIa-targeted chemotherapeutic agents for breast cancer. J. Med. Chem. 62, 8194-8234 (2019).

(2-Pyridyldithio)-PEG1-hydrazine is a one-unit cleavable polyethylene glycol (PEG) linker specifically designed for the synthesis of antibody-drug conjugates (ADCs). This linker offers the advantage of controlled release of the drug payload from the ADC construct. It is utilized in the conjugation process between the antibody and the cytotoxic drug, enabling the targeted delivery of the drug to cancer cells. The (2-pyridyldithio) group of this linker provides stability during circulation in the bloodstream, while the hydrazine moiety allows for efficient drug release at the tumor site. Overall, the (2-pyridyldithio)-PEG1-hydrazine linker serves as a valuable tool in the development of targeted chemotherapeutic agents for cancer treatment.

3Ac-SL0101 is a potent RSK-specific inhibitor. It facilitates the development of RSK inhibitors as anti-cancer chemotherapeutic agents.

CEP-6800 is a potent PARP inhibitor with potential anticancer activity. CEP-6800 could be used as a chemopotentiating agent with a variety of clinically effective chemotherapeutic agents.

Ki23057 is a a FGFR2 inhibitor, which enhances the chemosensitivity of drug-resistant gastric cancer cell lines when used in combination with chemotherapeutic drugs. Ki23057 might be therapeutically promising for treating drug-resistant gastric cancer cells, especially when used in combination with SN38, PTX, or VP16. The apoptosis process might be the main mechanism underlying the synergistic effect of these combinations. The ERCC1 and p53 genes may play an integral role in the synergism between Ki23057 and chemotherapeutic agents in drug-resistant cell lines. (source: Cancer Lett. 2011 Aug 1;307(1):47-52).

BIM-46068 is a potent and specific inhibitor of human farnesyltransferase. In regard to a panel of cell lines, using the Compare analysis to determine the Pearson coefficient correlation, the anti-proliferative spectrum of BIM-46068 has been shown to be distinct from the profile of typical chemotherapeutic agents.

1. Demethoxycurcumin (Desmethoxycurcumin) has antioxidant activity. 2. Demethoxycurcumin has anti-inflammatory activity. 3. Demethoxycurcumin has anti-proliferative activity. 4. Demethoxycurcumin has anti-acanthamoebic effect. 5. Demethoxycurcumin is a potential additive natural product in combination with chemotherapeutic agents in drug-resistant cancers. 6. Demethoxycurcumin inhibits energy metabolic and oncogenic signaling pathways through AMPK activation in triple-negative breast cancer cells.

Aurora kinase-IN-1, a potent aurora kinase inhibitor, modulates cell cycle progression and induces apoptosis by upregulating G1 cell cycle inhibitory proteins (including p21 and p27), elevating G1 progressive cyclin D1, and downregulating G1-to-S progressive cyclins, thereby arresting the cell cycle at the G1/S boundary. It stands as a promising lead compound for the development of chemotherapeutic agents.

Dalotuzumab (MK-0646) is a recombinant humanized IgG1 monoclonal antibody that specifically targets the insulin-like growth factor 1 receptor (IGF-1R). its mechanism of action involves the inhibition of IGF-mediated oncogenic signaling, which subsequently induces apoptosis and cell cycle arrest in tumor cells, and it has demonstrated enhanced antitumor efficacy when used in combination with other chemotherapeutic agents.

Tarextumab (OMP-59R5) is a fully human IgG2 monoclonal antibody designed to selectively target and inhibit the signaling of Notch2 and Notch3 receptors. preclinical and clinical studies have demonstrated that inhibition of the Notch2/3 pathway with chemotherapeutic agents is efficacious across a broad spectrum of epithelial tumors, including breast, lung, ovarian, and pancreatic cancers, thereby establishing Tarextumab as a promising candidate for oncological research and development.

Mal-PEG8-Val-Ala-PAB-Exatecan (Compound 9b), an antibody-drug conjugate linker (ADC linker), binds Nectin-4 polypeptides to chemotherapeutic agents for use in cancer research [1].

AEM1 is an inhibitor of deregulated NRF2 transcriptional activity in cancer. AEM1 acts by broadly decreasing the expression of NRF2 controlled genes, sensitizing A549 cells to various chemotherapeutic agents, and inhibiting the growth of A549 cells in vitro and in vivo.

Demethoxy Curcumin-d4 is a deuterated compound of Demethoxy Curcumin. Demethoxy Curcumin has a CAS number of 22608-11-3. 1. Demethoxycurcumin has antioxidant activity. 2. Demethoxycurcumin has anti-inflammatory activity. 3. Demethoxycurcumin has anti-proliferative activity. 4. Demethoxycurcumin has anti-acanthamoebic effect. 5. Demethoxycurcumin is a potential additive natural product in combination with chemotherapeutic agents in drug-resistant cancers. 6. Demethoxycurcumin inhibits energy metabolic and oncogenic signaling pathways through AMPK activation in triple-negative breast cancer cells.

Lup-20(29)-en-28-oic acid exhibits anticancer activities in various cancer types by inhibiting autophagic flux and synergistically enhancing the effectiveness of chemotherapeutic agents against HeLa cells. Pulsatilla saponin D demonstrates strong haemolytic activity.

(+)-Acuminatin exerts hepatoprotective activities, perhaps by serving as a potent antioxidant. (+)-trans-Acuminatin, and (+)-cis-acuminatin show weak activity against platelet aggregation with IC50 values of 108.5 and 90.02 uM, respectively. (+)-Acuminatin, and machilin G show dose-dependent potent inhibitory activities against PLCgamma1 in vitro with IC50 values ranging from 8.8 to 26.0 microM, the inhibition of PLCgamma1 may be an important mechanism for an antiproliferative effect on the human cancer cells, therefore, these inhibitors may be utilized as cancer chemotherapeutic and chemopreventive agents.

Dofequidar (MS-209 free base) is an orally active quinoline derivative that inhibits the efflux of chemotherapeutic agents and may overcome MDR by inhibiting ABCB1/P-gp, ABCC1/MDR-related protein 1, or both.