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

SJG-136 (dimer 5) is a DNA cross-linking agent, with an XL50 (concentration of agent required for 50% cross-linking of pBR322 DNA) of 45 nM for pBR322 DNA. SJG-136 is cytotoxic to ovarian cell lines, such as A2780 (IC50, 22.5 pM), A2780cisR (IC50, 24 pM), CH1 (IC50, 0.12 nM), CH1cisR (IC50, 0.6 nM), and SKOV-3 (IC50, 9.1 nM)[1]. SJG-136 (SG2000) also reduces the viability of a panel of canine cancer cells, with GI50 values ranging from 0.33 - >100 nM after a 1 h exposure, and <0.03 - 17.33 nM following continuous exposure[2].

SJG-136 shows more potent antitumor effect against CMeC-1 tumour at 0.30 mg/kg than 0.15 mg/kg either as a single dose or administered once a week for three weeks via dosed intravenously in mice. SJG-136-induced H2AX phosphorylation shows good correspondence, but less sensitivity, than measurement of foci[2].

[1]. Gregson SJ, et al. Design, synthesis, and evaluation of a novel pyrrolobenzodiazepine DNA-interactive agent with highly efficient cross-linking ability and potent cytotoxicity. J Med Chem. 2001 Mar 1;44(5):737-48. [2]. Mellinas-Gomez M, et al. Activity of the DNA minor groove cross-linking agent SG2000 (SJG-136) against canine tumours. BMC Vet Res. 2015 Aug 19;11:215.

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