SJG 136

XL50: 45 nM (pBR322 DNA)

SJG-136 (dimer 5) is a DNA cross-linking agent, with an XL ₅₀ (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 (IC ₅₀ , 22.5 pM), A2780cisR (IC ₅₀ , 24 pM), CH1 (IC ₅₀ , 0.12 nM), CH1cisR (IC ₅₀ , 0.6 nM), and SKOV-3 (IC ₅₀ , 9.1 nM). SJG-136 (SG2000) also reduces the viability of a panel of canine cancer cells, with GI ₅₀ values ranging from 0.33 - >100 nM after a 1 h exposure, and <0.03 - 17.33 nM following continuous exposure.

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.