SJG-136

SJG-136 is a DNA cross-linking agent, with an XL₅₀ of 45 nM for pBR322 DNA. SJG-136 has potent antitumor activity. IC50 & Target:XL50: 45 nM (pBR322 DNA)^[1] In Vitro: 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]. In Vivo: 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].