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Cat. No. Name Size Price Add Cart
KI1349TRC1021 g$60

Chemical Characteristic

Product NameTRC102
SynonymsMethoxyamine HCl
CAS No.593-56-6
Molecular Weight 83.51
FormulaCH6ClNO
Chemical NameMethoxyammonium chloride
SmilesNOC Cl
Chemical Structure

Biological activities

TRC102 is a small molecule inhibitor of base-excision repair (BER). TRC102 enhances the cytotoxicity of alkylator and antimetabolite chemotherapy and reverses chemotherapy resistance. TRC102 inhibits BER by binding apurinic (AP) sites produced by glycosylase removal of damaged DNA bases, thereby targeting them for cleavage by topoisomerase II and triggering apoptosis. [1] TRC102-AP sites have the ability to block the BER pathway and induce topo II-mediated DNA scission. [2] The addition of TRC102 on the aldehyde group at an AP site in vitro inhibits the alkaline rupture of the adjacent phosphodiester bond. TRC102 blocks specifically the cleavage by HeLa AP endonucleases. [3] TRC102 inhibits SW480 and HCT116 colon cancer cell lines with IC50 of 50 and 28 mM. TRC102 potentiates DNA single strand breaks and double strand breaks induced by temozolomide in colon cancer cells. [4]

Protocols

Stock solutions of TRC102 are prepared in water and stored at -20 °C. [3]

References

[1] SP Anthony, et al. A phase I study of daily oral TRC102 (methoxyamine) to enhance the therapeutic effects of pemetrexed in patients with advanced refractory cancer. J Clin Oncol. 2009.
[2] Yan L, et al. Combined treatment with temozolomide and methoxyamine: blocking apurininc/pyrimidinic site repair coupled with targeting topoisomerase IIalpha. Clin Cancer Res. 2007, 13(5): 1532-1539.
[3] Rosa S, et al. Processing in vitro of an abasic site reacted with methoxyamine: a new assay for the detection of abasic sites formed in vivo. Nucleic Acids Res. 1991, 19(20): 5569-5574.
[4] Taverna P, et al. Methoxyamine potentiates DNA single strand breaks and double strand breaks induced by temozolomide in colon cancer cells.Mutat Res. 2001, 485(4): 269-2681.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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