Amsacrine hydrochloride NEW
| Price | $39 | $54 | $72 |
| Package | 10mg | 25mg | 50mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-17 |
Product Details
| Product Name: Amsacrine hydrochloride | CAS No.: 54301-15-4 |
| Purity: 99.92% | Supply Ability: 10g |
| Release date: 2024/11/17 |
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. |
| 細胞實驗 | 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 various doses of amsacrine (0.5-12 mg kg(-1)), significant increases in micronucleated polychromatic erythrocytes were observed at 9 and 12 mg kg(-1), with higher doses causing significant suppression of erythroblast proliferation. Amsacrine exhibits high incidences of clastogenicity and low incidences of aneugenicity[2]. |
| 存儲條件 | 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) |
| 關鍵字 | inhibit | Inhibitor | acridinyl anisidide | Topoisomerase | Amsacrine Hydrochloride | Amsacrine hydrochloride | Amsacrine | acridinyl anisidide Hydrochloride | m-AMSA Hydrochloride | m-AMSA | Autophagy |
| 相關產(chǎn)品 | Hydroxychloroquine | Guanidine hydrochloride |
| 相關庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 抗癌上市藥物庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 抗癌藥物庫 | 抗癌活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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