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Tretazicar 98%

Tretazicar

源葉(MedMol)
S89139
21919-05-1
C9H8N4O5
252.18
品牌 貨號 產品規格 價格(RMB) 庫存（上海） 北京 武漢 南京 購買數量
源葉(MedMol) S89139-5mg 98% ￥146.00元 6 - - -
源葉(MedMol) S89139-10mg 98% ￥220.00元 6 - - -
源葉(MedMol) S89139-50mg 98% ￥710.00元 3 - - -
源葉(MedMol) S89139-200mg 98% ￥2550.00元 2 - - -
產品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產品

產品介紹

Tretazicar (CB 1954), an antitumor proagent, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involves the reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1)
產品描述： Tretazicar (CB 1954), an antitumor proagent, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involves the reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1)
靶點： DNA Alkylator/Crosslinker;DNAAlkylator/Crosslinker;?DNAAlkylation
體外研究：
Tretazicar (CB 1954) (0.1-1000 μM; 3 days) has sensitivity for retrovirally transduced AB22 (AB22-nr) cells with an IC50 of 3 μM.
DNA cross-link formation in affected cells is a result of the bioactivation of the drug by the enzyme DT diaphorase (NAD(P)H dehydro-genase (quinone)) in the Walker cells which reduces the 4-nitro group of Tretazicar. The product of this reaction is a difunctional alkylating agent, 5-aziridin-1-yl-4-hydroxylamino-2-nitrobenzamide。
體內研究：
Tretazicar (CB 1954) (80 mg/kg; i.p. on days 2 and 9) results in a significant increase in survival. Animal Model: Female BALB/c mice (AB22-nr, SKOV3 human ovarian tumour xenograft) Dosage: 80 mg/kg Administration: i.p. on days 2 and 9 Result: The median survival of the AB22-nr was 49 days. Resulted in a significant increase in survival.
參考文獻：
1. Knox RJ,et al. Bioactivation of 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB 1954) by human NAD(P)H quinone oxidoreductase 2: a novel co-substrate-mediated antitumor prodrug therapy. Cancer Res. 2000 Aug 1;60(15):4179-86. 2. Knox RJ, et al. CB 1954: from the Walker tumor to NQO2 and VDEPT. Curr Pharm Des. 2003;9(26):2091-104. 3. Green NK, et al. Immune enhancement of nitroreductase-induced cytotoxicity: studies using a bicistronicadenovirus vector. Int J Cancer. 2003 Mar 10;104(1):104-12. 4. Drabek D, et al. The expression of bacterial nitroreductase in transgenic mice results in specific cell killing by the prodrug CB1954. Gene Ther. 1997 Feb;4(2):93-100.
溶解性： Soluble  in  DMSO
保存條件： -20℃
配置溶液濃度參考：
1mg 5mg 10mg
1 mM 3.965 ml 19.827 ml 39.654 ml
5 mM 0.793 ml 3.965 ml 7.931 ml
10 mM 0.397 ml 1.983 ml 3.965 ml
50 mM 0.079 ml 0.397 ml 0.793 ml
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參考文獻

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