
SJG-136 NSC 694501
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SJG-136
SJG-136 (NSC 694501)是随机设计的PBD二聚体(pyrrolobenzodiazepine dimers),即将进入二期临床试验,用于治疗恶性疾病。NCI(National Cancer Institute)在60余种癌症细胞中测试发现,SJG-136显示细胞毒性强烈。
1 Thurston DE. Advances in the study of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) anti-tumour antibiotics Neidle S Waring MJ eds. . Topics in molecular and structural biology: molecular aspects of anticancer drug-DNA interactions, 1993p. 54-88, The Macmillan Press Ltd. London
2.Puvvada MS, Forrow SA, Hartley JA, et al Inhibition of bacteriophage T7 RNA polymerase in vitro transcription by DNA-binding pyrrolo[2,1-c][1,4]benzodiazepines. Biochemistry, 1997; 36: 2478-84,
CrossRefMedline
3.Gregson SJ, Howard PW, Jenkins TC, Kelland LR, Thurston DE. Synthesis of a novel C2/C2′-exo unsaturated pyrrolobenzodiazepine cross-linking agent with remarkable DNA binding affinity and cytotoxicity. J Chem Soc Chem Commun, 1999; 9: 797-8,
4.Gregson SJ, Howard PW, Hartley JA, 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; 44: 737-48,
5.Hartley JA, Spanswick VJ, Brooks N, et al SJG-136 (NSC 694501), a novel rationally designed DNA minor groove interstrand cross-linking agent with potent and broad spectrum anti-tumour activity. Part 1: cellular pharmacology, in vitro and initial in vivo antitumor activity. Cancer Res, 2004; 64: 6693-9,
6 Gregson, S.J., 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. 44(5): p. 737-48.
7. Hopton, S.R. and A.S. Thompson, Nuclear magnetic resonance solution structures of inter- and intrastrand adducts of DNA cross-linker SJG-136. Biochemistry, 2011. 50(21): p. 4720-32.
8. Alley, M. C., M. G. Hollingshead, et al. (2004). "SJG-136 (NSC 694501), a novel rationally designed DNA minor groove interstrand cross-linking agent with potent and broad spectrum antitumor activity: part 2: efficacy evaluations." Cancer Res 64(18): 6700-6706.
SJG-136 (NSC 694501)是随机设计的PBD二聚体(pyrrolobenzodiazepine dimers),即将进入二期临床试验,用于治疗恶性疾病。NCI(National Cancer Institute)在60余种癌症细胞中测试发现,SJG-136显示细胞毒性强烈。
CAS: 232931-57-6
同义词: SJG 136;SP-2001;BN 2629;NSC 694501。Pyrrolo[2,1-c][1,4]benzodiazepine dimer;1,1'- [[(propane-1,3-diyl)dioxy]bis[(11aS)-7-methoxy-2-methylidene- 1,2,3,11a-tetrahydro-5H-pyr- rolo[2,1-c][1,4]benzodiazepin-5-one]]; (10Z,10'Z,11aS,11a'S)-8,8'-(propane-1,3-diylbis(oxy))bis(7-methoxy-2- methylene-2,3-dihydro-1H-benzo[e]pyrrolo[1,2-a][1,4]diazepin- 5(11aH)-one)。
IUPAC/Chemical name:(11aS,11a'S)-8,8'-(propane-1,3-diylbis(oxy))bis(7-methoxy-2-methylene-2,3-dihydro-1H-benzo[e]pyrrolo[1,2-a][1,4]diazepin-5(11aH)-one)
分子式:C31H32N4O6
分子量:M.t. 556.61
| 货号 | 产品名称 | 化学结构式 | 分子式 | 纯度 | 价格(US $) |
| D1004 | SJG-136 | C31H32N4O6 M.t. 556.61 |
95% | Inquiry | |
1 Thurston DE. Advances in the study of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) anti-tumour antibiotics Neidle S Waring MJ eds. . Topics in molecular and structural biology: molecular aspects of anticancer drug-DNA interactions, 1993p. 54-88, The Macmillan Press Ltd. London
2.Puvvada MS, Forrow SA, Hartley JA, et al Inhibition of bacteriophage T7 RNA polymerase in vitro transcription by DNA-binding pyrrolo[2,1-c][1,4]benzodiazepines. Biochemistry, 1997; 36: 2478-84,
CrossRefMedline
3.Gregson SJ, Howard PW, Jenkins TC, Kelland LR, Thurston DE. Synthesis of a novel C2/C2′-exo unsaturated pyrrolobenzodiazepine cross-linking agent with remarkable DNA binding affinity and cytotoxicity. J Chem Soc Chem Commun, 1999; 9: 797-8,
4.Gregson SJ, Howard PW, Hartley JA, 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; 44: 737-48,
5.Hartley JA, Spanswick VJ, Brooks N, et al SJG-136 (NSC 694501), a novel rationally designed DNA minor groove interstrand cross-linking agent with potent and broad spectrum anti-tumour activity. Part 1: cellular pharmacology, in vitro and initial in vivo antitumor activity. Cancer Res, 2004; 64: 6693-9,
6 Gregson, S.J., 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. 44(5): p. 737-48.
7. Hopton, S.R. and A.S. Thompson, Nuclear magnetic resonance solution structures of inter- and intrastrand adducts of DNA cross-linker SJG-136. Biochemistry, 2011. 50(21): p. 4720-32.
8. Alley, M. C., M. G. Hollingshead, et al. (2004). "SJG-136 (NSC 694501), a novel rationally designed DNA minor groove interstrand cross-linking agent with potent and broad spectrum antitumor activity: part 2: efficacy evaluations." Cancer Res 64(18): 6700-6706.
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