鹽酸胺苯吖啶|T5820|TargetMol

價(jià)格	￥139	￥297	￥497
包裝	1mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-29

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產(chǎn)品詳情

中文名稱:鹽酸胺苯吖啶	英文名稱:Amsacrine hydrochloride
CAS:54301-15-4	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.92%	產(chǎn)品類別: 抑制劑
貨號(hào): T5820

Product Introduction

Bioactivity

名稱	Amsacrine hydrochloride
描述	Amsacrine hydrochloride (acridinyl anisidide hydrochloride) is topoisomerase II inhibitor , is used in the treatment of acute myelogenous leukemia.
細(xì)胞實(shí)驗(yàn)	Voltage-clamp measurements of Xenopus oocytes were performed in a solution containing (in mM): 5 KCl, 100 NaCl, 1.5. CaCl2, 2 MgCl2 and 10 HEPES (pH adjusted to 7.4 with NaOH). Current and voltage electrodes were filled with 3 m KCl solution.?For whole-cell patch-clamp recordings from HEK 293 cells, electrodes were filled with the following solution (in mM): 130 K-aspartate, 5.0 MgCl2, 5 EGTA, 4 ATP, 10 HEPES (pH adjusted to 7.2 with KOH). The external solution for these experiments contained (in mM): 137 NaCl, 4.0 KCl, 1.0 MgCl2, 1.8 CaCl2, 10 HEPES, 10 glucose (pH adjusted to 7.4 with NaOH).?Amsacrine was prepared as 10 mm stock solution in DMSO and stored at -20℃. On the day of experiments, aliquots of the stock solution were diluted to the desired concentrations with the bath solution. HERG current amplitudes (recorded from Xenopus oocytes) were not significantly altered upon application of 1% DMSO (v v^-1; maximum bath concentration) for 20 min. In addition, DMSO did not affect HERG channel currents recorded from HEK 293 cells at concentrations up to 0.3% (maximum bath concentration in this study: 0.1% DMSO)[1].
體外活性	Amsacrine hydrochloride blocked HERG currents in HEK 293 cells and Xenopus oocytes in a concentration-dependent manner, with IC50 values of 209.4 nm and 2.0 microm, respectively. HERG channels were primarily blocked in the open and inactivated states, and no additional voltage dependence was observed. Amsacrine caused a negative shift in the voltage dependence of both activation (-7.6 mV) and inactivation (-7.6 mV). HERG current block by amsacrine was not frequency dependent. The S6 domain mutations Y652A and F656A attenuated (Y652A) or abolished (F656A, Y652A/F656A) HERG current blockade, indicating that amsacrine binding requires a common drug receptor within the pore-S6 region[1].
體內(nèi)活性	In animals treated with different doses of amsacrine (0.5-12 mg kg(-1) ), the frequencies of micronucleated polychromatic erythrocytes increased significantly after treatment with 9 and 12 mg kg(-1) . caused significant suppressions of erythroblast proliferation at higher doses.amsacrine has high incidences of clastogenicity and low incidences of aneugenicity[2].
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 4.3 mg/mL (10 mM)
關(guān)鍵字	inhibit \| Inhibitor \| acridinyl anisidide \| Topoisomerase \| Amsacrine Hydrochloride \| Amsacrine hydrochloride \| Amsacrine \| acridinyl anisidide Hydrochloride \| m-AMSA Hydrochloride \| m-AMSA \| Autophagy
相關(guān)產(chǎn)品	Guanidine hydrochloride \| Hydroxychloroquine
相關(guān)庫	抑制劑庫 \| 經(jīng)典已知活性庫 \| 抗癌上市藥物庫 \| 抗癌活性化合物庫 \| 抗衰老化合物庫 \| 藥物功能重定位化合物庫 \| 抗癌臨床化合物庫 \| 抗癌藥物庫

關(guān)鍵字： acridinyl anisidide hydrochloride|||鹽酸胺苯吖啶|||m-AMSA hydrochloride|TargetMol

公司簡(jiǎn)介

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