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Amonafide
  • Amonafide

Amonafide

價格 977.75
包裝 1EA
最小起訂量 1EA
發(fā)貨地 其他
更新日期 2020-01-12

產(chǎn)品詳情

英文名稱:AmonafideCAS:69408-81-7
規(guī)格: 10mg/10mM/1mL/50mg/100mg貨號: S1367
2020-01-12 Amonafide Amonafide 1EA/977.75RMB 977.75
Selleck Chemicals美國品牌,中國庫存現(xiàn)貨,Topoisomerase抑制劑,CAS#69408-81-7。
更多詳情請訪問中國唯一官方網(wǎng)站: http://www.selleck.cn/products/Amonafide.html


?

生物活性

產(chǎn)品描述 Amonafide (NSC-308847)通過topoisomerase II(拓撲異構(gòu)酶II)介導(dǎo)導(dǎo)致蛋白相關(guān)的DNA鏈斷裂,但不會產(chǎn)生拓撲異構(gòu)酶I介導(dǎo)的DNA裂解。Phase 3。
靶點 Topoisomerase II ? ? ? ? ?
IC50 ? ? ? ? ? ?
體外研究 Through a topoisomerase II-mediated reaction, Amonafide treatment produces DNA single-strand breaks (SSB), double-strand breaks (DSB), and DNA-protein cross-links in human myeloid leukemia cells. Amonafide treatment inhibits conlony formation of the leukemic cell lines and the normal human bone marrow GM-CFC in a dose-dependent manner. Amonafide does not produce topoisomerase I-mediated DNA cleavage even at 100 μM. The m-AMSA-resistant line is less than 2-fold resistant to Amonafide?

[1]

?Amonafide interferes with the DNA breakage-reunion activity of mammalian DNA topoisomerase II resulting in DNA cleavage stimulation.?

[2]

?Compared with those of other antitumor drugs, Amonafide-stimulated cleavage intensity patterns are markedly different. Amonafide highly prefers a cytosine, and excludes guanines and thymines instead, at position -1, with lower preference for an adenine at position +1.?

[3]

?Topoisomerase II-mediated DNA cleavage induced by Amonafide is affected only slightly (less than 3-fold) by 1 mM ATP, suggeting that Amonafide is an ATP-insensitive topoisomerase II inhibitor in contrast to doxorubicin, etoposide, and mitoxantrone.?

[4]

?Amonafide significantly inhibits the growth of HT-29, HeLa, and PC3 cells with IC50 of 4.67 μM, 2.73 μM, and 6.38 μM, respectively.?

[5]

?Amonafide is unaffected by P-glycoprotein-mediated efflux, unlike those of the classical topoisomerase II inhibitors (daunorubicin, doxorubicin, idarubicin, etoposide, and mitoxantrone).?

[6]

體內(nèi)研究 ?
臨床實驗 A Phase I/II study of Amonafide in men with androgen-independent prostate cancer has been completed.
特征 ?

細胞試驗:?

[5]

細胞系 HT-29, HeLa, and PC3
濃度 Dissolved in DMSO, final concentrations ~10 μM
處理時間 72 hours
方法 All cell lines are in the logarithmic phase of growth when the assay of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) is carried out. Cells are harvested and seeded into 96-well tissue culture plates at a density of 2.5 × 103?cells/well in 150 μL aliquots of medium. The concentrations tested are serial dilutions of a stock solution (10 μM in DMSO) with phosphate-buffered saline (PBS) and are added 24 hours later. The assay is ended after 72 hours of Amonafide exposure and PBS is used as a negative control. After 72 hours treatment, cells are washed twice with PBS, and then 50 μL/well of MTT reagent (1 mg/mL in PBS) together with 150 μL/well of prewarmed medium are added. The plates are returned to the incubator for 4 hours. Subsequently, DMSO is added as solvent. Absorbance is determined at 570 nm with a Microplate reader. All experiments are performed at least three times, and the average of the percentage absorbance is plotted against concentration. Then, the concentration of Amonafide required to inhibit 50% of cell growth (IC50) is calculated for Amonafide.
溫馨提示:不可用于臨床治療。
關(guān)鍵字: Amonafide;化學試劑

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