SJG-136 - CAS 232931-57-6

SJG-136 - CAS 232931-57-6 Catalog number: BADC-00825

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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.

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BADC-00825 -- $--
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; SJG136; SJG-136; SP-2001; SP2001; SP 2001; BN 2629; BN2629; BN-2629; SG2000; SG 2000; SG-2000; NSC 694501; NSC694501; NSC-694501
Canonical SMILES
DMSO: ≥ 100 mg/ml
In Vitro
SJG-136 was highly potent in the colon cancer cell lines HCT-116, HT-29 and SW620 (IC50 0.1-0.3 nM). However, HCT-8 and HCT-15 cells expressing significant levels of mdr-1 were less sensitive (IC50 2.3 and 3.7 nM, respectively) using a SRB assay. The cytotoxicity was increased in HCT-15 and A2780(AD) in presence of 5 microg/ml verapamil. Mdr-1 mRNA expression was determined by qRT-PCR and correlated to SJG-136 IC50s (r2=0.86, P=0.0001). Isogenic 3T3 cells expressing mdr-1 cDNA (3T3 pHamdr-1) were less sensitive to SJG-136 than the parental 3T3 cells (IC50 208 and 6.3 nM, respectively). Finally, SJG-136 (120 microg/kg/d dx5) was highly active against A2780 xenografts (SGD=275) but not A2780(AD) xenografts (SGD=67).
In Vivo
The pharmacokinetics and in vitro metabolism of SJG-136 and as well as the feasibility of using the Comet assay to measure in vivo interstrand DNA cross-links, was assessed in the rat. SJG-136 half-life, clearance and volume of distribution values were 9 min, 190 ml/min/m(2), and 1780 ml/m(2), respectively. SJG-136 did not accumulate in plasma during treatment with 25 μg/kg/day for 5 days. Treatment with SJG-136 produced the anticipated DNA interstrand cross-links, as well as DNA strand breaks, in rat PBMCs. Oxidative metabolism of SJG-136 in rat liver microsomes was catalyzed by CYP3A isoforms and produced a previously unreported monomeric metabolite.
Clinical Trial Information
NCT NumberCondition Or DiseasePhaseStart DateSponsorStatus
NCT00103220Unspecified Adult Solid Tumor, Protocol SpecificPhase 12013-12-11National Cancer Institute (NCI)Completed
NCT00121290Unspecified Adult Solid Tumor, Protocol SpecificPhase 12014-02-24National Cancer Institute (NCI)Completed
NCT00301769Adult Acute Myeloid Leukemia With 11q23 (MLL) AbnormalitiesPhase 12013-09-30National Cancer Institute (NCI)Terminated
NCT01200797Recurrent Fallopian Tube CancerPhase 22015-05-25National Cancer Institute (NCI)Terminated (Slow accrual was the reason for study termination.)
Shelf Life
0-4℃ for short term (days to weeks), or -20℃ for long term (months).
Room temperature
Store at -5°C,keep in dry and avoid sunlight.
Current Developer
Ipsen Inc
1.Nuclear magnetic resonance solution structures of inter- and intrastrand adducts of DNA cross-linker SJG-136.
Hopton SR1, Thompson AS. Biochemistry. 2011 May 31;50(21):4720-32. doi: 10.1021/bi102017e. Epub 2011 May 3.
SJG-136 (1) is a sequence-selective DNA-interactive agent that is about to enter phase II clinical trials for the treatment of malignant disease. Previous studies on the pyrrolo[2,1-c][1,4]benzodiazepine (PBD) dimers, typified by SJG-136 and DSB-120 (2), have shown that these planar ligands react with the exocyclic NH(2) groups of two guanine bases in the base of the minor groove of DNA to form an irreversible interstrand cross-linked sequence-specific adduct. Using high-field NMR, we have characterized and modeled the previously predicted interstrand duplex adduct formed by SJG-136 with the self-complementary 5'-d(CICGATCICG)(2) duplex (4). This first SJG-136 NMR-refined adduct structure has been compared with previous high-field NMR studies of the adducts of the closely related PBD dimer DSB-120 with the same duplex and of the adduct of tomaymycin (3) formed with 5'-d(ATGCAT)(2). Surprisingly, the SJG-136 duplex adduct appears to be more closely related to the tomaymycin adduct than to the DSB-120 adduct with respect of the orientation and depth of insertion of the ligand within the minor groove.
2.γ-H2AX foci formation as a pharmacodynamic marker of DNA damage produced by DNA cross-linking agents: results from 2 phase I clinical trials of SJG-136 (SG2000).
Wu J1, Clingen PH, Spanswick VJ, Mellinas-Gomez M, Meyer T, Puzanov I, Jodrell D, Hochhauser D, Hartley JA. Clin Cancer Res. 2013 Feb 1;19(3):721-30. doi: 10.1158/1078-0432.CCR-12-2529. Epub 2012 Dec 18.
PURPOSE: To evaluate γ-H2AX foci as a pharmacodynamic marker for DNA damage induced by DNA interstrand cross-linking drugs.
3.Activity of the DNA minor groove cross-linking agent SG2000 (SJG-136) against canine tumours.
Mellinas-Gomez M1,2, Spanswick VJ3, Paredes-Moscosso SR4, Robson M5, Pedley RB6, Thurston DE7,8, Baines SJ9,10, Stell A11, Hartley JA12. BMC Vet Res. 2015 Aug 19;11:215. doi: 10.1186/s12917-015-0534-2.
BACKGROUND: Cancer is the leading cause of death in older dogs and its prevalence is increasing. There is clearly a need to develop more effective anti-cancer drugs in dogs. SG2000 (SJG-136) is a sequence selective DNA minor groove cross-linking agent. Based on its in vitro potency, the spectrum of in vivo and clinical activity against human tumours, and its tolerability in human patients, SG2000 has potential as a novel therapeutic against spontaneously occurring canine malignancies.

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