AST-3424 (OBI-3424, TH-3424) is a first-in-class, novel prodrug that selectively targets cancers overexpressing the enzyme AKR1C3, OBI-3424 is a highly selective prodrug that is converted by AKR1C3 to a DNA alkylating agent.

Bisantrene is a highly effective antitumor drug, targets eukaryotic type II topoisomerases.

Carboplatin is a chemotherapy drug by binding to DNA and interfering with the cell's repair mechanism.

Cisplatin is an inorganic platinum agent (cis-diamminedichloroplatinum) with antineoplastic activity.

Cyclophosphamide is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic and immunosuppressive activities.

Ifosfamide is a nitrogen mustard alkylating agent used in the treatment of cancer.

Melphalan(Sarcolysin; L-PAM) is a chemotherapy drug belonging to the class of nitrogen mustard alkylating agents; attaches the alkyl group to the guanine base of DNA.

Methazolastone (Temozolomide, Temodar, Temodal) is a DNA damage inducer.

Mitomycin C is a DNA crosslinking agent that inhibits DNA synthesis and induces apoptosis in a variety of cells.

N,N’N’-triethylenethiophosphoramide (ThioTEPA) is a cancer chemotherapeutic member of the alkylating agent group.

Oxaliplatin is a second generation potent platinum-based anti-neoplastic agent that is believed to form inter- and intrastrand DNA adducts which activate signaling pathways culminating in apoptosis. The development of Oxaliplatin was inspired from the eff

TH-302 is selective hypoxia-activated prodrug targeting hypoxic regions of solid tumors with IC50 of 19 nM, demonstrates 270-fold enhanced cytotoxicity under hypoxia versus their potency under aerobic conditions, stable to cytochrome P450 metabolism.

Trabectedin (Ecteinascidin-743 or ET-743) is a novel antitumour agent of marine origin with potent antitumour activity both in vitro and in vivo.

Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen hydrochloride shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen hydrochloride induces irreversible DNA damage and cytotoxicity in MM cells.

4-Hydroperoxy cyclophosphamide is the active metabolite form of the prodrug Cyclophosphamide. 4-Hydroperoxy cyclophosphamide crosslinks DNA and induces T cell apoptosis independent of death receptor activation, but activates mitochondrial death pathways through production of reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide is used to treat lymphomas and autoimmune disorders.

Illudin M is a cytotoxic fungal sesquiterpene that can be isolated from the culture medium of Omphalotus olearius mushrooms. Illudin M can alkylate DNA. Illudin M has anti-tumor activities.

PIP-199 is a selective inhibitor of RMI (RecQ-mediated genome instability protein) core complex/MM2 interaction, with an IC50 of 36 μM. MM2 is the binding site of RMI complex on Fanconi anemia complementation group M protein (FANCM). PIP-199 can be used for the research of sensitizing resistant tumors to DNA crosslinking chemotherapeutics.

Duocarmycin DM, a DNA minor-groove alkylator, is an antibody drug conjugates (ADCs) toxin. Duocarmycin DM is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity.

Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties.

Phenylacetic acid mustard is the major metabolite of the cancer chemotherapeutic agent Chlorambucil. Chlorambucil is an alkylating agent with antitumor activity.

Phosphoramide mustard is the major metabolite for Cyclophosphamide, with anticancer activitiy. Phosphoramide mustard induces DNA adduct formation in ovarian granulosa cells, induces DNA damage and elicits the ovarian DNA repair response.

Phosphoramide mustard cyclohexanamine is the major metabolite for Cyclophosphamide, with anticancer activitiy. Phosphoramide mustard cyclohexanamine induces DNA adduct formation in ovarian granulosa cells, induces DNA damage and elicits the ovarian DNA repair response.

Busulfan-D8 is a deuterium labeled Busulfan. Busulfan is an alkyl sulfonate that acts as an alkylating antineoplastic agent. Busulfan forms both intra- and interstrand crosslinks on DNA. In mammals, Busulfan causes profound and prolonged reduction in the generation of hematopoietic progenitors without significantly affecting lymphocyte levels or humoral antibody responses.

Treosulfan (NSC 39069, Treosulphan) is an alkylating agent used for conventional and high-dose chemotherapy regimens. Treosulfan is potently cytotoxic against pancreatic cancer cell lines.

PR-104A (SN 27858) is the alcohol metabolite of phosphate prodrug PR-104. PR-104A is a hypoxia-selective DNA cross-linking agent/DNA-damaging agent and cytotoxin. Antitumor Activity. PR-104A is metabolized under hypoxia by the 1-electron NADPH:cytochrome P450 oxidoreductase. PR-104A can be used for the research of relapsed/refractory T-lineage acute lymphoblastic leukemia (T-ALL).

PR-104 is a selective hypoxia-activated DNA cross-linking agent can be used for the research of multiple tumor xenograft models. PR-104 as a nitrogen mustard pre-prodrug is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A.

PR-104 (sodium) is a selective hypoxia-activated DNA cross-linking agent can be used for the research of multiple tumor xenograft models. PR-104 (sodium) as a nitrogen mustard pre-prodrug is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A.

Lurbinectedin D3 is deuterium labeled Lurbinectedin. Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.

Sibiromycin is a naturally produced glycosylated pyrrolobenzodiazepines (PBDs). Sibiromycin is also a potent antitumor antibiotic that binds covalently to DNA in the minor groove at the NH2 of guanine.

(-)-Irofulven (MGI 114), an Illudin S analog, is a DNA alkylating agent. (-)-Irofulven inhibits the replication of DNA, induces tumor cells apoptosis, and has potent antitumor activity.

Mipicoledine is a potential neuro-alkylating agent for study of glioblastoma and metastatic cancers involving the central nervous system.

Methylnitronitrosoguanidine (MNNG) is an alkylating agent with toxic and mutagenic effects.

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

Colibactin 742, a stable colibactin derivative, induces DNA interstrand-cross-links, activation of the Fanconi Anemia DNA repair pathway, and G2/M arrest.

Lurbinectedin D3 is deuterium labeled Lurbinectedin. Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.

Porfiromycin is a bioreductive alkylating agent that preferentially kill hypoxic tumor cells relative to other aerobic counterparts.

EC2629 is a highly potent folate receptor (FR)-targeted DNA crosslinking agent. EC2629 can be used for the research of FR-positive tumors, including those that are classified as drug resistant.

Methyl methanesulfonate (MMS), a DNA alkylating agent, modifies both guanine (to 7-methylguanine) and adenine (to 3-methlyladenine) to cause base mispairing and replication blocks, respectively.

Duocarmycin analog-2 is a potent DNA alkylating agent. Duocarmycin analog-2 can be used of synthetic immunoconjugate. Duocarmycin analog-2 has antitumor activity.

LP-284 is a potent DNA alkylating agent that kills solid tumours. LP-284 can be used in the studies of hematologic cancers with compromised DNA repair, such as mantle cell lymphoma (MCL).

Prednimustine (Leo 1031;NSC 134087) is the ester formed from Prednisolone and Chlorambucil. Prednimustine can be used for leukemias and lymphomas research.

Ranimustine (MCNU) is a nitrosourea alkylating agent, can be used for research of chronic myelogenous leukemia and polycythemia vera.

SG2057 (DRG16) is a PBD dimer containing a pentyldioxy linkage which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts. SG2057 is a highly active antitumor agent.

OBI-3424 S-isomer (TH-3424, OBI 3424) is a highly potent DNA alkylating prodrug that is converted by AKR1C3 to a potent DNA-alkylating agent.

CDEAH is a monofunctional alkylating agent that selectively kills PARP1- and xeroderma pigmentosum A-deficient cells.

NSC373981 (NSC 373981) is a CARD11 G-quadruplex (G4) stabilizing small molecule that downregulates CARD11 gene expression in DLBCL cells.

QBS10072S is a novel dual-function, BBB permeable chemotherapeutic agent with alkylating moiety and a selective large neutral amino acid transporter 1 (LAT1, SLC7A5) substrate, shows excellent BBB penetration and promising efficacy in vitro (U251 cell IC5