nci-h522

LP-261 is a novel tubulin targeting anticancer agent that binds at the colchicine site on tubulin, inducing G2/M arrest.

Cyclophosphamide is an alkylating agent type of anti-tumor drug, and its main target is DNA. Cyclophosphamide inhibits the proliferation of tumor cells by undergoing alkylation reactions with DNA, interfering with the replication and transcription processes of DNA.

Cetzole (Compound 1) acts as an inducer of ferroptosis (iron-dependent cell death) through the accumulation of ROS, leading to cell death. The compound exhibits varying half-maximal cytotoxic concentrations (CC50) against several cell lines: 2.56 μM in NCI-H522, 10.31 μM in NCI-H522 GFP-SCL7A11 #8, 2.71 μM in NCI-H522 RV-GFP, 3.07 μM in HT-1080, 14.9 μM in NARF2, and 6.28 μM in MDA-MB-231. This highlights Cetzole's potential for research in cancer therapeutics.

EGFR-IN-160 is an EGFR inhibitor with IC50 values of 1.62, 0.49, and 0.98 μM for EGFRWT, EGFRT790M, and EGFRL858R/T790M/C797S, respectively. It can induce cell cycle arrest at the G2/M and S phases and apoptosis (Apoptosis) in NCI-H522 cells, demonstrating anticancer properties. Additionally, EGFR-IN-160 exhibits antioxidant activity against DPPH (IC50: 12.11 µM) and H2O2 (IC50: 8.89 µM).

Beta-Hydroxyisovalerylshikonin is an inhibitor of protein-tyrosine kinases such as v-Src and EGFR, and has been shown to induce apoptosis in several human tumor cell lines. Beta-Hydroxyisovalerylshikonin significantly decreased viability of HCT116 cells (IC50 values = 30.9 μg/mL).