dna alkylating

CEP-40125 (RXDX-107) is a DNA alkylating agent used for researching advanced solid tumors.

Oxaliplatin (L-OHP) is a DNA alkylating agent, an inhibitor of DNA synthesis. Oxaliplatin causes DNA cross-linking damage, preventing DNA replication and transcription and leading to cell death. Oxaliplatin induces autophagy.

Temozolomide (TMZ) is a DNA alkylating agent with blood-brain barrier permeability and oral activity. Temozolomide has antitumor activity and antiangiogenic activity, and also induces apoptosis and autophagy. Temozolomide is stable under acidic conditions and hydrolyzes under neutral or slightly alkaline conditions.

Sarmustine (SarCNU) is an alkylating agent with anticancer activity that inhibits the growth of prostate cancer cells via p53-dependent and p53-independent pathways.Sarmustine mediates the selection of P140K methylguanine-DNA-methyltransferase-transduced human CD34(+) cells in vitro.

Semustine, a DNA alkylating agent, is a cancer chemotherapy compound that is nephrotoxic in patients with malignant melanoma receiving adjuvant chemotherapy for the adjuvant treatment of leukemia.

Ecomustine is a water-soluble nitrosoureido sugar derived from acosamine, with alkylating activity. Ecomustine is a novel antitumor compound that alkylates and crosslinks DNA, thereby inhibiting replication and transcription and eventually resulting in a reduction of cellular proliferation.

Cyclophosphamide hydrate is a DNA alkylating agent, an inhibitor of DNA synthesis. Cyclophosphamide hydrate has antitumor and immunosuppressive activities.

Altretamine (ENT-50852) is an alkylating agent with antineoplastic activity.

Bendamustine hydrochloride (EP-3101) (IC50 of 50 μM) is an alkylating agent associated with DNA damage.

Lomustine (NSC-79037) is an alkylating agent of value against both hematologic malignancies and solid tumors.

Methoxyamine HCl (Methoxyamine) covalently binds to apurinic apyrimidinic (AP) DNA damage sites and inhibits base excision repair (BER), which may result in an increase in DNA strand breaks and apoptosis. Methoxyamine is an orally bioavailable small molecule inhibitor with potential adjuvant activity. This agent may potentiate the anti-tumor activity of alkylating agents.

N-Nitroso-N-methylurea is a nitrosourea compound with alkylating, carcinogenic and mutagenic properties. It targets a variety of animal organs, causes various cancers and degenerative diseases, and can be used in diazomethane synthesis.

Satraplatin (BMS182751) is an orally available antineoplastic platinum(IV) complex.Satraplatin has a favorable toxicity profile and appears to have clinical activity against a variety of malignancies.

Monohydroxy melphalan is a DNA alkylating agent and a degradation product of melphalan . Monohydroxy melphalan is formed by the hydrolysis of melphalan in aqueous solutions, including cell culture medium and human plasma. It increases the level of DNA adducts in ML-1 myeloblastic leukemia cells in a concentration-dependent manner and induces cytotoxicity with an IC50 value of 28.1 μg/ml.

OBI-3424, a highly selective prodrug, is converted by aldo-keto reductase family 1 member C3 (AKR1C3) to a potent DNA-alkylating agent.

Bendamustine D4 is the deuterium-labeled Bendamustine. Bendamustine is a DNA cross-linking compound with alkylating and antimetabolite properties. Bendamustine causes DNA breaks.

DGN462 is an effective DNA alkylating agent with anti-tumor activity, as in acute myeloid leukemia (AML). DGN462 can be used as a cytotoxic component of antibody-drug conjugates (ADCs).

DC1 can be used to synthesize antibody-drug conjugates targeted to the treatment of cancer, is an ADC cytotoxin, similar to the small groove-binding DNA alkylating agent CC-1065.

(+)-CBI-CDPI1, an enhanced functional analog of CC-1065, is a DNA alkylating agent and an antibody-drug conjugate (ADCs) toxin.

Vc-seco-DUBA is a drug-linker conjugate for ADC with potent antitumor activity by using DUBA (DNA alkylating agent), linked via the ADC linker Vc-seco[1].

Aniline-MPB-amino-C3-PBD is a cytotoxic agent with a non-alkylating group and acts as a sequence-selective DNA minor-groove binding agent.

Duocarmycin MB, an antibody-drug conjugate (ADCs) toxin, is a DNA alkylating agent that binds in the minor groove and can be used against multi-drug resistant cell lines.

Caricotamide is a synthetic co-substrate that activates the human endogenous enzyme NRH:quinone oxidoreductase 2 (NQO2) with potential chemoadjuvant activity. When caricotamide is administered simultaneously with the prodrug tretazicar, NQO2 converts tretazicar to the bifunctional alkylating agent dinitrobenzamide, which is capable of forming a high degree of DNA interstrand cross-links, resulting in the inhibition of DNA replication and the induction of apoptosis. NQO2 has been found to be over-expressed in cancers such as hepatocellular carcinoma (HCC), colorectal and ovarian cancers.

Duocarmycin analog-2, a potent DNA alkylating agent, exhibits antitumor effects and can be utilized in the synthesis of immunocouplers.