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Amsacrine hydrochloride

Catalog No. T5820 CAS 54301-15-4

Synonyms: acridinyl anisidide hydrochloride, m-AMSA hydrochloride

Amsacrine hydrochloride (acridinyl anisidide hydrochloride) is topoisomerase II inhibitor , is used in the treatment of acute myelogenous leukemia.

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Amsacrine hydrochloride Chemical Structure

Amsacrine hydrochloride, CAS 54301-15-4

Pack Size	Availability	Price/USD
10 mg	In stock	$ 39.00
25 mg	In stock	$ 54.00
50 mg	In stock	$ 72.00
100 mg	In stock	$ 97.00
200 mg	In stock	$ 126.00
500 mg	In stock	$ 178.00
1 g	In stock	$ 262.00
1 mL * 10 mM (in DMSO)	In stock	$ 29.00

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Purity: 99.71%

Purity: 99.62%

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Description	Amsacrine hydrochloride (acridinyl anisidide hydrochloride) is topoisomerase II inhibitor , is used in the treatment of acute myelogenous leukemia.
In vitro	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].
In vivo	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].
Cell Research	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].

Synonyms	acridinyl anisidide hydrochloride, m-AMSA hydrochloride
Molecular Weight	429.92
Formula	C21H20ClN3O3S
CAS No.	54301-15-4

Storage

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

Solubility Information

DMSO: 4.3 mg/mL (10 mM)

References and Literature

1. Thomas D , Hammerling B C , Wu K , et al. Inhibition of cardiac HERG currents by the DNA topoisomerase II inhibitor amsacrine: mode of action[J]. British Journal of Pharmacology, 2004, 142(3):485-494. 2. Attia S M . Molecular cytogenetic evaluation of the mechanism of genotoxic potential of amsacrine and nocodazole in mouse bone marrow cells[J]. Journal of Applied Toxicology, 2013, 33(6).

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Inhibitor Library Approved Drug Library DNA Damage & Repair Compound Library Bioactive Compounds Library Max Autophagy Compound Library

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Keywords

Amsacrine hydrochloride 54301-15-4 Autophagy DNA Damage/DNA Repair Topoisomerase inhibit acridinyl anisidide hydrochloride Inhibitor acridinyl anisidide Amsacrine Hydrochloride Amsacrine acridinyl anisidide Hydrochloride m-AMSA Hydrochloride m-AMSA hydrochloride m-AMSA inhibitor

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