DNA Alkylator/Crosslinker Inducer

Hepsulfam (NCI 329680; ZINC01574758) is a anticancer agent that shows excellent antileukemic activity with an median IC₅₀ of 0.91 μg/mL in a panel of different tumors.

QBS10072S is a LAT1-selective substrate with blood-brain barrier permeability that inhibits tumor growth. QBS10072S enters LAT1-expressing tumor cells via LAT1-mediated active transport, induces interstrand DNA cross-linking and cell apoptosis, and reduces leptomeningeal dissemination. QBS10072S can be used in studies related to glioblastoma multiforme, diffuse intrinsic pontine glioma, triple-negative breast cancer brain metastases, and aggressive T-cell lymphoma.

Sunitinib-platinum(IV) prodrug-1 (Complex A) is a Pt(IV) prodrug based on Cisplatin (HY-17394), and this design aims to enable Pt(IV) to be reduced to active Pt(II) under intracellular reducing conditions, while simultaneously releasing a derivative of Sunitinib (HY-10255A) with tyrosine kinase inhibitor (TKI) activity. Sunitinib-platinum(IV) prodrug-1 exhibits excellent cytotoxicity against renal cell carcinoma (RCC), causing DNA crosslinking and apoptosis. Sunitinib-platinum(IV) prodrug-1 inhibits the VEGFR/PDGFR signaling pathway, suppressing tumor growth and angiogenesis. Sunitinib-platinum(IV) prodrug-1 can be used for research on renal cell carcinoma.

Anti-CCL2 (Carlumab)-MC-Vc-PAB-DMEA-PEG2-Duocarmycin SA is an antibody-drug conjugate (ADC) consisting of the humanized anti-CCL2 (chemokine ligand 2) antibody Carlumab (HY-P99188) conjugated with the linker MC-Vc-PAB-DMEA-PEG2 and the DNA alkylator Duocarmycin SA (HY-12456). Anti-CCL2 (Carlumab)-MC-Vc-PAB-DMEA-PEG2-Duocarmycin SA can be used in cancer research.

SG3683 is a DNA-targeted cytotoxic agent belonging to pyrrolobenzodiazepine (PBD) dimers. SG3683 exerts antitumor activity with an IC₅₀ value of 0.74 nM in MDA-MB-436 cells. SG3683 is promising for research of cancers, such as breast cancer.

FK 973 is a dihydrobenzoxazine anticancer agent. FK 973 selectively inhibits DNA synthesis and can form DNA cross-links through cytoplasmic activation. FK 973 exhibits significant antitumor activity in various animal tumor models and human tumor xenografts, with relatively weak myelosuppressive effects. FK 973 is sensitive to neural tumor cells. FK 973 can be used for DNA-targeted antitumor research.

HJ03 is a blood-brain barrier-permeable, orally active DNA damage and ferroptosis inducer. HJ03 triggers ferroptosis by increasing intracellular ROS, Fe²⁺ accumulation and lipid peroxidation. HJ03 induces DNA adducts and interstrand crosslinks, blocks DNA replication and transcription, arrests cells at the G2/M phase and induces apoptosis. HJ03 can be used in the research of glioblastoma multiforme and colorectal cancer.

QBS10072S dihydrochloride is a LAT1-selective substrate with blood-brain barrier permeability that inhibits tumor growth. QBS10072S dihydrochloride enters LAT1-expressing tumor cells via LAT1-mediated active transport, induces interstrand DNA cross-linking and cell apoptosis, and reduces leptomeningeal dissemination. QBS10072S dihydrochloride can be used in studies related to glioblastoma multiforme, diffuse intrinsic pontine glioma, triple-negative breast cancer brain metastases, and aggressive T-cell lymphoma.

Aminoflavone is an anti-tumor agent. Aminoflavone inhibits the expression of ITGA6/SOX2 by activating the AhR-miR-125b-2-3p axis, thereby targeting breast cancer stem cells. Aminoflavone induces an increase in intracellular ROS, increases the level of oxidative DNA damage marker 8-oxodG and DNA-protein cross-links. Aminoflavone causes S-phase arrest, activates caspase-3/8/9 and induces apoptosis (apoptosis). Aminoflavone inhibits HIF-1α expression in a manner independent of AhR. Aminoflavone can be used for the study of breast cancer.

Anticancer agent 11 is a broad-spectrum anticancer agent that inhibits angiogenesis and induces DNA cross-links.

Hepsulfam (NCI 329680; ZINC01574758) is a anticancer agent that shows excellent antileukemic activity with an median IC50 of 0.91 μg/mL in a panel of different tumors.