alkylating

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.

Carmustine (bis-chloroethylnitrosourea) is a cell-cycle phase nonspecific alkylating antineoplastic agent.

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

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

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

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

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.

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.

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.

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.

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

Aniline mustard (Mesylerythrol) is alkylating mustard with anti-neoplastic activity.

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.

APE1-IN-1 is a potent inhibitor of purine pyrimidine endonuclease 1 (APE1) that crosses the blood-brain barrier, exhibits potential antitumor activity, and enhances the cytotoxicity of the alkylating agent [methyl methanesulfonate] on cancer cells.

Cyclophosphamide is an alkylating agent used in the treatment of several forms of cancer including leukemias, lymphomas and breast cancer.

Evofosfamide (TH-302) is a hypoxia-activated prodrug of the cytotoxin bromo-isophosphoramide mustard (Br-IPM) conjugated with 2-nitroimidazole, possessing potential antineoplastic activity. Under hypoxic conditions, typical of hypoxic tumors, the 2-nitroimidazole moiety is reduced, releasing the DNA-alkylating Br-IPM moiety, which induces intra- and inter-strand DNA crosslinks that inhibit DNA replication and cell division, potentially causing apoptosis in tumor cells. The inactive form of the prodrug remains stable under normoxic conditions, which may reduce systemic toxicity.

Bendamustine (SDX105) for the treatment of Non-Hodgkin Lymphomas and Chronic Lymphocytic Leukemia

Temozolomide Acid (TMZA) is a metabolite of temozolomide (TMZ). Temozolomide processes anticancer activity in vitro. Temozolomide (TMZ) is an oral alkylating agent used to treat glioblastoma multiforme (GBM) and astrocytomas.

Treosulfan (Treosulphan) is a bifunctional alkylating agent. It also has activity in ovarian cancer and other solid tumor types.

Lobaplatin (D-19466) (D-19466) is a diastereometric mixture of platinum(II) complexe. Lobaplatin (D-19466) is a third-generation platinum anti-neoplastic agent which shows activity for a variety of tumour types and is a promising antitumour chemotherapeutic agent[1][2]. It is a platinum complex with DNA alkylating activity.

VAL-083 is an alkylating agent with antitumor activity that produces N7 methylation on DNA.

Cyclophosphamide-d4 is a deuterated compound of Cyclophosphamide. Cyclophosphamide has a CAS number of 50-18-0. Cyclophosphamide is an alkylating agent used in the treatment of several forms of cancer including leukemias, lymphomas and breast cancer.

Acrylamide-2,3,3-d3 is a deuterated compound of Acrylamide. Acrylamide has a CAS number of 79-06-1. Acrylamide is a member of the class of acrylamides. It has a role as a carcinogenic agent, a neurotoxin, a mutagen, an alkylating agent and a Maillard reaction product

Estromustine is a major active metabolite of the cystotatic estrogen and nitrogen mustard alkylating antineoplastic agent estramustine phosphate, used in the therapy of prostate cancer.

Enpromate is a synthetic acetyl carbamate, nitrogen mustard compound. It is an alkylating agent with antitumor activity.

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.

Kenazepine is a benzodiazepine cpd containing functional alkylating moiety.

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

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.

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

Iodoacetamide, an alkylating agent, is commonly utilized for cysteine alkylation in proteomics sample preparation.

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.

Melphalen fluoroaniline, also known as melphalen, J-1, or prodrug J-1, is a prodrug of melphalen, in which the alkylating agent melphalen is combined with fluoroaniline and has potential antitumor and antiangiogenic activities.

Pipobroman (Vercyte) is an anti-cancer drug that probably acts as an alkylating agent. Pipobroman has well documented clinical activity in polycythemia vera (PV) and essential thrombocythemia (ET). Pipobroman allows, within 3 months, to attain a response in more than 90% of patients, without clinically relevant toxicities. The 10-years risk of thrombosis of patients treated with Pipobroman is about 15%, The anti-proliferative activity of Pipobroman on bone marrow megakaryocytes seems of particular value in lowering the occurrence of post-PV and post-ET MMM, whose risk is the lowest registered with available treatments. The 10-year risk of acute leukemia with Pipobroman is 5% in PVand 3% in ET, which is only slightly higher than that expected as a natural evolution of the disease. In conclusion, the use of Pipobroman is a definite alternative to hydroxyurea in patients with PV and ET at high risk of thrombosis.

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

Piposulfan, a water-insoluble alkylating agent, is used as an antineoplastic and anti-tumor agent.

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

CB1954(Tretazicar (NSC-115829)), an anticancer prodrug, is activated by NAD(P)H quinone oxidoreductase 2. It is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent.

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).

Ethylene dimethanesulfonate has selective pro-apoptotic effects on LCs. Ethylene dimethanesulfonate is a mild alkylating, non-volatile methanesulfonic diester of ethylene glycol. 

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.

Ranimustine (MCNU) can be used for polycythemia vera and chronic myelogenous leukemia research, which is a nitrosourea alkylating agent [1] [3] [4].

LP-284 is a potent DNA alkylating agent that kills solid tumors and can be used in hematologic cancer studies with compromised DNA repair, such as mantle cell lymphoma (MCL) [1] [2].

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].

GYKI-13324 is bifunctional nitrosoureido derivative and alkylating agent. GYKI-13324 was studied on human colorectal tumor xenograft lines. Given orally in single or multiple daily doses, GYKI-13324 produced long-term or total regression of adenomatous, b

Epipropidine is an epoxide, which is an alkylating agent with antitumor activity, LD50 intravenous in mouse: 74mg/kg. it is not used clinically due to its unstable nature.

Sarcolysine hydrochloride, also known as Melphalan HCl, is a nitrogen mustard and alkylating agent that has been studied for use in multiple myeloma therapy.

Nemorubicin HCL is the salt form of Nemorubicin, also known as PNU152243A, a doxorubicin derivative that differs significantly from its parent drug in terms of spectrum of antitumor activity, metabolism and toxicity profile. The drug is active on tumors resistant to alkylating agents, topoisomerase II inhibitors and platinum derivatives. It works primarily through topoisomerase I inhibition. Of note, Nemorubicin is active in cells with upregulation of the nucleotide excision repair (NER) pathway, where current therapies fail. Nemorubicin is biotransformed in the liver into cytotoxic metabolites that may further contribute to render this drug highly active against primary liver tumors or liver metastases.

Melflufen (Melphalan flufenamide) hydrochloride, an alkylating agent and dipeptide prodrug of Melphalan, exhibits antitumor activity by inducing irreversible DNA damage and cytotoxicity in multiple myeloma (MM) cells, while also inhibiting angiogenesis.