4t1 breast cancer cells

WRG-28 is a potent and selective, allosteric discoidin domain receptor 2 (ddr2) inhibitor(IC50 : 230 nM)

CAR-2 is a BODIPY-based photosensitizer that induces ferroptosis in photodynamic therapy (PDT) by targeting the endoplasmic reticulum (ER) and lipid droplets (LD). It exhibits phototoxicity against breast cancer cells with an IC50 of 0.01-0.02 μM and demonstrates antitumor efficacy in a 4T1 xenograft mouse model.

Anti-TNBC agent-8 (Compound TP2) is a photodynamic therapeutic compound that targets mitochondrial DNA G-quadruplexes (mtG4). Under white light exposure, it exhibits an IC50 of 0.42 μM against 4T1 cells. Anti-TNBC agent-8 tightly binds to mtG4, leading to the production of substantial reactive oxygen species (ROS) under illumination. This results in the loss of mitochondrial membrane potential (MMP), reduced ATP production, elevated ROS levels, and significant apoptosis in triple-negative breast cancer (TNBC) cells, thus demonstrating its tumor growth inhibitory activity. Anti-TNBC agent-8 is applicable for research in TNBC.

FGT-4 is a chimeric molecule targeting folate receptor β (FR-β) and functions as a TLR7 agonist. It enhances the secretion of iNOS and the pro-inflammatory cytokine IL-6 associated with M1 macrophages and promotes the proliferation of cytotoxic CD8+ T cells. FGT-4 demonstrates antitumor activity in the 4T1 breast cancer mouse model and is applicable for cancer immunotherapy research.

PI3K-IN-59 (Compound 3d) is a PI3K inhibitor with an IC50 value of 17.44 μM. It demonstrates significant antiproliferative activity, showing potent inhibition against breast cancer 4T1 cells (IC50: 3.70 μM), colon cancer CT26 cells (IC50: 1.98 μM), and human breast cancer cells (IC50: 19.72 μM). The compound operates through a dual antitumor mechanism by inhibiting PI3Kα enzymatic activity and inducing hydroxyl radical (•OH) generation via the Fenton reaction. PI3K-IN-59 shows promising efficacy against 4T1 tumors, making it suitable for synergistic targeting studies in breast and colon cancer.

Fluoxetine-Conjugated Platinum(IV) prodrug-1 is an eEF2K inhibitor that can hinder the proliferation of cancer cells, induce DNA damage, and cause cell cycle arrest at the S phase, leading to apoptosis (Apoptosis). It also promotes the accumulation of reactive oxygen species (ROS) and disrupts mitochondrial function. This prodrug inhibits the migration and invasion of TNBC cells by suppressing MMP-2 activity and induces autophagy in TNBC cells through AMPK activation. In the 4T1-Luc mouse model, it exhibits antitumor activity and triggers immune suppression. Fluoxetine-Conjugated Platinum(IV) prodrug-1 is relevant for research in triple-negative breast cancer (TNBC).

PROTACPD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with significant PD-L1 protein degradation capacity. It demonstrates strong PD-L1 degradation activity in 4T1 cells, with a DC50 of 0.609 μM. This compound is applicable to breast cancer research.

pro-FTY is an anticancer prodrug of FTY720 and acts as a sphingosine-1-phosphate (S1P) inhibitor. It specifically inhibits S1P signaling in cancer cells via a drug delivery system (DDS) that reacts with acrolein. pro-FTY significantly reduces the survival of breast cancer cells, including multidrug-resistant cells and organoids resistant to Paclitaxel or Doxorubicin. Additionally, pro-FTY effectively suppresses tumor growth in xenograft mouse models of 4T1 cells or organoids while avoiding lymphopenia.

GSK484-Ph (compound 15d) is an analog of GSK484, exhibiting potent anti-cancer activity. It effectively inhibits 4T1 cells and can be utilized in breast cancer research.

PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer. 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3/Akt PH domain binding, that is designed for more favorable solubility in vivo. 3,5-dimethyl PIT-1 inhibits PI3K/Akt signaling (IC50 = 27 μM), suppressing PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 36 μM). 4T1 breast cancer growth is significantly attenuated in BALB/c mice with a dose of 1 mg/kg of 3,5-dimethyl PIT-1 per day.

Nifuroxazide-d4 is intended for use as an internal standard for the quantification of nifuroxazide by GC- or LC-MS. Nifuroxazide is a nitrofuran antibiotic. It is active against strains of the enteropathogenic bacteria C. jejuni, Salmonella, Y. enterocolitica, Shigella, and E. coli. It inhibits quorum sensing and virulence factor production in P. aeruginosa. Nifuroxazide inhibits STAT3 activity in a reporter assay and decreases viability of U266 and INA-6 myeloma cells, which have constitutive STAT3 phosphorylation, with EC50 values of approximately 4.5 µM for both. It also decreases viability, migration, and invasion of, and induces apoptosis in, MCF-7, 4T1, and MDA-MB-231 breast cancer cells. Nifuroxazide reduces tumor growth and prevents pulmonary metastasis in a 4T1 murine mammary carcinoma model. It also reduces diarrhea, weight loss, and colon inflammation in a rat model of acetic acid-induced ulcerative colitis.

Antitumor agent-115 (SS-12) is a potent anti-tumor compound with an IC50 range of 0.34 μM-24.14 μM against the 4T1 mouse breast cancer cell line. It impedes the cell cycle, diminishes mitochondrial membrane potential, and triggers apoptosis, with an IC50 for cell viability spanning 8-25 μmol/L. This compound is applicable in breast cancer research [1].

HDAC3-IN-2 (compound 4i), a pyrazinyl hydrazide-based HDAC3 inhibitor with an IC50 of 14 nM, effectively targets triple-negative breast cancer cells. Demonstrating cytotoxic activity, HDAC3-IN-2 exhibits an IC50 of 0.55 μM against 4T1 cells and 0.74 μM against MDA-MB-231 cells. In vivo, it shows anti-tumor efficacy in tumor-bearing mouse models by selectively elevating acetylation of histones H3K9, H3K27, and H4K12, enhancing apoptosis-inducing proteins caspase-3, caspase-7, and cytochrome c, and diminishing proliferation markers Bcl-2, CD44, EGFR, and Ki-67 [1].

Anticancer agent 33 (compound 3), derived from Squamocin and Bullatacin, exhibits potent inhibitory activity against the 4T1 breast cancer cell line (A549, HeLa, HepG2, and MCF-7 cells) with IC50 values ranging from 1.9 to 5.4 µM [1].

LLK203 is a potent dual-target inhibitor of USP2/USP8 with IC50 values of 0.89 μM and 0.52 μM, respectively. It promotes ERα degradation and induces apoptosis in breast cancer MCF-7 cells, demonstrating antitumor activity in the 4T1 tumor mice model [1].