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Diaziquone

Catalog No. T61383 CAS 57998-68-2

Synonyms: NSC 182986

Diaziquone (NSC-182986) is a water-soluble synthetic azacyclic benzoquinone that enhances penetration of the blood-brain barrier, has antitumor activity, and is used in the treatment of extreme renal failure.

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Diaziquone, CAS 57998-68-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 188.00
5 mg	In stock	$ 470.00
10 mg	In stock	$ 689.00
25 mg	In stock	$ 1,080.00
50 mg	In stock	$ 1,460.00
100 mg	In stock	$ 1,960.00
500 mg	In stock	$ 3,930.00

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Purity: 98.37%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Diaziquone (NSC-182986) is a water-soluble synthetic azacyclic benzoquinone that enhances penetration of the blood-brain barrier, has antitumor activity, and is used in the treatment of extreme renal failure.
In vitro	Diaziquone (5000 ng/mL) is associated with prolonged aplasia and rare instances of bone marrow necrosis, but only mild extramedullary toxicity. One- and three-hour treatments produced little cytotoxicity for hematopoietic versus marrow stromal cells. After six-hour treatments with this dose, marrow was depleted of CFU-Mix, BFU-E, and CFU-GM, but produced CFU-GM in LTMCs, indicating an ongoing input of CFU-GM from a surviving pre-CFU-Mix population. Diaziquone (150 ng/mL; 3 to 7 days) elimination of the latter may be inferred from the absence of CFU-GM in the LTMCs exposed.[4]
In vivo	Diaziquone (0.1 mg/day; injection; 4 days) applied topically in Vanicream, Plastibase, or DMSO inhibited tumor growth at day 20 by 66, 86, and 43%, respectively, and cured animals of the skin tumor at a dose of 0.5 mg/day. Diaziquone administered i.p. at 0.5 mg/day for 4 days was lethal to rats, and at 0.1 mg/day it produced 93% inhibition of tumor growth at day 20. Diaziquone was applied topically at 0.1 mg/day for 4 days in Plastibase-cured rats of advanced tumors when treatment was begun 12 days after injection of tumor cells. The area under the plasma radioactivity time curve over 5 h for a single 0.64-mg dose of topically applied [ring-14C]diaziquone in DMSO was 0.01% that of the same dose of [ring-14C]diaziquone administered i.p. in non-tumored rats. The decrease in WBC count following topical application of diaziquone at a dose of 0.1 mg/day for 4 days, compared to the same dose of diaziquone administered i.p., was 62% in Vanicream, 81% in Plastibase and 33% in DMSO. Topical diaziquone was non-toxic to normal skin in the rat and in the domestic pig. It is concluded that topical application of diaziquone offers a therapeutic advantage over systemic treatment for metastatic cancer of the skin.[2]

Synonyms	NSC 182986
Molecular Weight	364.35
Formula	C16H20N4O6
CAS No.	57998-68-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (123.51 mM)

References and Literature

1. Schold SC Jr, et al. Treatment of human glioma and medulloblastoma tumor lines in athymic mice with diaziquone and diaziquone-based drug combinations. Cancer Res. 1984;44(6):2352-2357. 2. Moore DJ, et al. Topical chemotherapy of intradermal Walker 256 carcinosarcoma with diaziquone and doxorubicin in the rat. Cancer Res. 1985;45(11 Pt 1):5466-5472. 3. Lee EJ, et al. Diaziquone given as a continuous infusion is an active agent for relapsed adult acute nonlymphocytic leukemia. Blood. 1986;67(1):182-187. 4. Kushner BH, et al. Myeloablation with diaziquone: in vitro assessment. Blood. 1987;69(6):1747-1752. 5. Gutierrez PL, et al. Free radicals in quinone containing antitumor agents. The nature of the diaziquone (3,6,-diaziridinyl-2,5-bis(carboethoxyamino)-1,4-benzoquinone) free radical. Biochim Biophys Acta. 1983;758(1):37-41. 6. White L. Responsiveness of retinoblastoma to local diaziquone. Studies in a xenograft model. Invest Ophthalmol Vis Sci. 1990;31(5):787-791.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Bioactive Compound Library

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Keywords

Diaziquone 57998-68-2 NSC 182986 NSC-182986 NSC182986 inhibitor inhibit

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