Exatecan mesylate | Topoisomerase I inhibitor

Exatecan mesylate chemical structure

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Exatecan mesylate (169869-90-3) is a hexacyclic, water soluble camptothecin analog exhibiting potent antitumor activity in vitro and in vivo.1 It is a potent topoisomerase I inhibitor displaying antiproliferative activity against 32 malignant cell lines and was shown to be 6 and 28 times more potent than SN-38 and topotecan respectively1. It displays potent cytotoxic effects in various drug-resistant cells.2 Exatecan can be utilized as a cytotoxic payload in the development of novel antibody drug conjugates (ADCs).3

References/Citations:

  1. Mitsui et al. (1995) A new water-soluble camptothecin derivative, DX-8951f, exhibits potent antitumor activity against human tumors in vitro and in vivo; Jpn. J. Cancer Res., 86 776
  2. Ishii et al. (2000) Growth inhibitory effect of a new camptothecin analog, DX-8951f, on various drug-resistant sublines including BCRP-mediated camptothecin derivative-resistant variants derived from the human lung cancer cell line PC-6; Anticancer Drugs, 11 353
  3. Nakata et al. (2016) Novel antibody drug conjugates containing exatecan derivative-based cytotoxic payloads; Bioorg. Med. Chem. Lett., 26 1542
169869-90-3, ADC payload, exatecan mesylate, Exatecan mesylate supplier, exatecan supplier, toposiomerase I inhibitor
Alternate Name:
DX-8951f

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Exatecan mesylate (169869-90-3) is a hexacyclic, water soluble camptothecin analog exhibiting potent antitumor activity in vitro and in vivo.1 It is a potent topoisomerase I inhibitor displaying antiproliferative activity against 32 malignant cell lines and was shown to be 6 and 28 times more potent than SN-38 and topotecan respectively1. It displays potent cytotoxic effects in various drug-resistant cells.2 Exatecan can be utilized as a cytotoxic payload in the development of novel antibody drug conjugates (ADCs).3

References/Citations:

  1. Mitsui et al. (1995) A new water-soluble camptothecin derivative, DX-8951f, exhibits potent antitumor activity against human tumors in vitro and in vivo; Jpn. J. Cancer Res., 86 776
  2. Ishii et al. (2000) Growth inhibitory effect of a new camptothecin analog, DX-8951f, on various drug-resistant sublines including BCRP-mediated camptothecin derivative-resistant variants derived from the human lung cancer cell line PC-6; Anticancer Drugs, 11 353
  3. Nakata et al. (2016) Novel antibody drug conjugates containing exatecan derivative-based cytotoxic payloads; Bioorg. Med. Chem. Lett., 26 1542