DNA alkylator

DNA alkylators are a class of compounds that can add alkyl groups (e.g., methyl or ethyl groups) to the DNA molecule, leading to DNA damage. This modification can result in mispairing or prevention of DNA replication, which can lead to cell death. Given their ability to damage DNA, alkylating agents are used as chemotherapy drugs to treat various cancers. However, their use can also be associated with significant side effects, as they can damage normal cells in addition to cancer cells. Popular examples of alkylating agents include cyclophosphamide, melphalan, and busulfan.


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  1. Altretamine is classified as an alkylating antineoplastic agent.This unique structure is believed to damage tumor cells through the production of the weakly alkylating species formaldehyde, a product of CYP450-mediated N-demethylation.
  2. Bendamustine Hydrochloride is a small molecule bifunctional DNA alkylating agent, combining a nitrogen mustard functionality with a purine-analog structure. The dense DNA-damaging functionality of Bendamustine differentiates it from other compounds used as antiproliferative agents, and these functionalities are thought to promote cell death through a variety of different pathways including apoptosis and mitotic catastrophe.

  3. Thiotepa is a polyfunctional, organophosphorus alkylating agent and a stable derivative of N,N',N''-triethylenephosphoramide (TEPA), with antineoplastic activity.
  4. Procarbazine Hydrochloride is an alkylating agent, with anticancer activity.
  5. Cyclophosphamide monohydrate is an alkylating, cytotoxic agent experimentally shown to crosslink DNA, causing strand breakage and inducing mutations.
  6. Palifosfamide is a synthetic mustard compound with potential antineoplastic activity.
  7. Uramustine is a chemotherapy drug which belongs to the class of alkylating agents.
  8. Miriplatin hydrate is a lipophilic platinum complex containing myristates as leaving groups, and can be easily suspended in ethyl esters of iodized fatty acids obtained from poppy seed oil.
  9. bi-functional alkylating agent

    VAL-083 is a bi-functional alkylating agent; inhibit U251 and SF188 cell growth in monolayer better than TMZ and caused apoptosis.
  10. DNA alkylating agent

    Melphalan is a cytotoxic drug used to treat multiple myeloma. Phenylamine derivative of mechorethamine.
  11. Azoxymethane is a colon carcinogen which leads to the formation of DNA adducts.
  12. DNA/RNA Alkylator

    Carmustine is an antitumor chemotherapeutic agent, which works by akylating DNA and RNA.
  13. Nimustine hydrochloride is an antineoplastic agent especially effective against malignant brain tumors. The resistance which brain tumor cells acquire to the initial effectiveness of this drug can be partially overcome by the simultaneous use of membrane-modifying agents such as reserpine, calcium antagonists such as nicardipine or verapamil, or the calmodulin inhibitor, trifluoperazine.
  14. Lurbinectedin (PM01183) is a new 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.
  15. Treosulfan (NSC 39069;Treosulphan) is an alkylating agent with activity in ovarian cancer and other solid tumor types.
  16. Methylnitronitrosoguanidine (MNNG) is an alkylating agent with toxic and mutagenic effects.
  17. DNA alkylating agent

    (+)-CBI-CDPI2 is an enhanced functional analog of CC-1065. (+)-CBI-CDPI1 is a DNA alkylating agent. (+)-CBI-CDPI2 is an antibody drug conjugates (ADCs) toxin.
  18. DNA alkylating agent

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

    Duocarmycin GA is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin GA can be used against multi-drug resistant cell lines.
  20. DNA alkylator

    Duocarmycin TM is an exceptionally potent antitumor antibiotic. Duocarmycin TM is a DNA alkylator.
  21. DNA alkylator

    DC41 is a DC1 derivative. DC1, a simplified analogue of CC-1065, is an antibody conjugate of cytotoxic DNA alkylators for the targeted treatment of cancer.
  22. DNA alkylator

    DC41SMe, a DC1 derivative, shows cytotoxicity in Ramos, Namalwa, and HL60/s cells with IC50s ranging from 18-25 pM. DC1, a simplified analogue of CC-1065, is an antibody conjugate of cytotoxic DNA alkylators for the targeted treatment of cancer.
  23. DNA alkylator

    DC1, an analogue of the minor groove-binding DNA alkylator CC-1065, is an antibody conjugate of cytotoxic DNA alkylators for the targeted treatment of cancer.
  24. DNA alkylator

    DC1Sme, a DC1 derivative, exhibits IC50 values of 22 pM, 10 pM, 32 pM and 250 pM for Ramos, Namalwa, HL60/s and COLO 205 cancer cells, respectively. DC1, a simplified analogue of CC-1065, is an antibody conjugate of cytotoxic DNA alkylators for the targeted treatment of cancer.
  25. alkylating agent

    Satraplatin is an alkylating agent, with potent antitumor effect.
  26. DNA cross-linking agent

    SJG-136 is a DNA cross-linking agent, with an XL50 of 45 nM for pBR322 DNA. SJG-136 has potent antitumor activity.
  27. DNA alkylator

    Duocarmycin A, which is one of well-known antitumor antibiotics, is a DNA alkylator and efficiently alkylates adenine N3 at the 3?? end of AT-rich sequences in the DNA.
  28. DNA alkylator

    Semustine is a DNA alkylator, binds to DNA, and acts as a cancer chemotherapeutic agent.

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