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Banoxantrone dihydrochloride (AQ4N dihydrochloride)

  • 產(chǎn)品貨號:CS-01Y70634
  • 產(chǎn)品價(jià)格:電議
  • 產(chǎn)品產(chǎn)地:進(jìn)口、國產(chǎn)
  • 包裝類型:10mM*1mLinWater 5mg 25mg
  • 采購熱度:273
  • 庫存:100
  • CAS號:252979-56-9
  • 方法:
  • 含量:>99.00%
  • 品牌名稱:莼試
  • 分子式:C22H30Cl2N4O6
  • 分子量:517.4

簡介內(nèi)容:質(zhì)量保證、價(jià)格優(yōu)惠

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標(biāo)簽:Banoxantrone dihydrochloride (AQ4N dihydrochloride) 

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化學(xué)性質(zhì):                                                                                                             

規(guī)格

10mM*1mLinWater 5mg 25mg

CAS

252979-56-9

別名

N/A

化學(xué)名

N/A

分子式

C22H30Cl2N4O6

分子量

517.4

溶解度

H2O : 25 mg/mL (48.32 mM)

儲存條件

Store at -20°C,

General tips

For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

 

產(chǎn)品描述:                                                                                                            

Banoxantrone dihydrochloride is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.

Banoxantrone (AQ4N) can be reduced in a hypoxic environment to a stable DNA-affinic agent AQ4. AQ4, a potent topoisomerase II inhibitor, would be capable of damaging cells recruited into the cell cycle following radiation damage to the well-oxygenated cells of the tumor[1]. Banoxantrone shows more than 8-fold higher cytotoxicity under hypoxia than normoxia in cultures of 9L rat gliosarcoma and H460 human non-small-cell lung carcinoma cells but not for 11 other human cancer cell lines. DT-diaphorase protein levels and banoxantrone chemosensitivity are poorly correlated across the cancer cell line panel, and banoxantrone chemosensitivity is not affected by DT-diaphorase inhibitors[2]. Banoxantrone is a bis-N-oxide that is reduced via two sequential two-electron reductions to the tertiary amine, AQ4, which is a potent cytotoxic agent toward both aerobic and hypoxic cells. AQ4, but not AQ4N, intercalates in DNA with high affinity to generate a stable persistent complex that can inhibit topoisomerase II and cause DNA damage and cell death[3].

Banoxantrone (200 mg/kg) significantly enhances the tumor growth delay caused by radiation. This occurred when radiation is administered both as a single dose (12 Gy) and in a multifraction regimen (5x3 Gy). A study of the scheduling of Banoxantrone (AQ4N) administration shows that there is a very long time period over which a maximal effect can be elicited (drug given 4 days before to 6 h after radiation). These results suggest that Banoxantrone has significant potential as a bioreductive drug[1]. The activation of banoxantrone cytotoxicity in vivo requires tumor hypoxia that is more extensive or prolonged than can readily be achieved by vasodilation or by antiangiogenic drug treatment[2]. Incorporation of banoxantrone into conventional chemoradiation protocols therefore targets both oxygenated and hypoxic regions of tumors, and potentially will increase the effectiveness of therapy. A single dose of 60 mg/kg banoxantrone enhances the response of RT112 (bladder) and Calu-6 (lung) xenografts to treatment with cisplatin and radiation therapy. Banoxantrone will increase the efficacy of chemoradiotherapy in preclinical models[3].

[1]. Hejmadi MV, et al. DNA damage following combination of radiation with the bioreductive drug AQ4N: possible selective toxicity to oxic and hypoxic tumour cells. Br J Cancer. 1996 Feb;73(4):499-505. [2]. Manley E Jr, et al. Impact of tumor blood flow modulation on tumor sensitivity to the bioreductive drug banoxantrone. J Pharmacol Exp Ther. 2013 Feb;344(2):368-77. [3]. Williams KJ, et al. In vivo activation of the hypoxia-targeted cytotoxin AQ4N in human tumor xenografts. Mol Cancer Ther. 2009 Dec;8(12):3266-75.

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原創(chuàng)作者:上海莼試生物技術(shù)有限公司

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