1. Cell Cycle/DNA Damage
    Autophagy
  2. Topoisomerase
    Autophagy
  3. Amsacrine hydrochloride

Amsacrine hydrochloride (Synonyms: m-AMSA hydrochloride; acridinyl anisidide hydrochloride)

Cat. No.: HY-13551A Purity: 98.98%
Handling Instructions

Amsacrine hydrochloride (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.

For research use only. We do not sell to patients.

Amsacrine hydrochloride Chemical Structure

Amsacrine hydrochloride Chemical Structure

CAS No. : 54301-15-4

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 66 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 110 In-stock
Estimated Time of Arrival: December 31
100 mg USD 140 In-stock
Estimated Time of Arrival: December 31
500 mg USD 220 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Amsacrine hydrochloride (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.

IC50 & Target[1]

Topoisomerase II

 

In Vitro

Amsacrine (mAMSA) blocks HERG currents in HEK 293 cells and Xenopus oocytes in a concentration-dependent manner, with IC50 values of 209.4 nM and 2.0 μM, respectively. Amsacrine (mAMSA) causes a negative shift in the voltage dependence of both activation (−7.6 mV) and inactivation (−7.6 mV). HERG current block by Amsacrine (mAMSA) is not frequency dependent[1]. In vitro studies of normal human lymphocytes with various concentrations of Amsacrine (mAMSA), show both increased levels of chromosomal aberrations, ranging from 8% to 100%, and increase SCEs, ranging from 1.5 times the normal at the lowest concentration studied (0.005 μg/mL) to 12 times the normal (0.25 μg/mL)[3]. Amsacrine (mAMSA)-induced apoptosis of U937 cells is characterized by caspase-9 and caspase-3 activation, increased intracellular Ca2+ concentration, mitochondrial depolarization, and MCL1 down-regulation. Amsacrine induces MCL1 down-regulation by decreasing its stability. Further, amsacrine-treated U937 cells show AKT degradation and Ca2+-mediated ERK inactivation[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In animals treated with different doses of amsacrine (0.5-12 mg/kg), the frequencies of micronucleated polychromatic erythrocytes increase significantly after treatment with 9 and 12 mg/kg. Furthermore, the present study demonstrates for the first time that Amsacrine (mAMSA) has high incidences of clastogenicity and low incidences of aneugenicity whereas nocodazole has high incidences of aneugenicity and low incidences of clastogenicity during mitotic phases in vivo[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

429.92

Formula

C₂₁H₂₀ClN₃O₃S

CAS No.
SMILES

CS(=O)(NC1=CC=C(NC2=C(C=CC=C3)C3=NC4=CC=CC=C42)C(OC)=C1)=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (145.38 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3260 mL 11.6301 mL 23.2601 mL
5 mM 0.4652 mL 2.3260 mL 4.6520 mL
10 mM 0.2326 mL 1.1630 mL 2.3260 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.84 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

Mice[2]
Amsacrine (mAMSA) is investigated in three separated experiments. In the first experiment, animals are treated by intraperitoneal injection with 0.5, 1.5 and 4.5 mg/kg of Amsacrine (mAMSA) and bone marrow is sampled 24 h after treatment. Preliminary negative MN results at this sampling time lead to the use of 30 h sampling time for Amsacrine (mAMSA). Thus, in the second experiment, mice are treated with 0.5, 1.5 and 4.5 mg/kg of Amsacrine (mAMSA) and bone marrow is sampled 30 h after treatment. The doses and sampling times for Amsacrine are chosen by reference to earlier studies and the selected doses are within the dose range used for human chemotherapy. The results again show that the micronuclei frequency in the bone marrow of mice is not affected by treatment with any of the selected doses of the test agent, at 30 h sampling time, thus, in the third experiment, mice are treated with 6, 9 and 12 mg/kg of Amsacrine and bone marrow is sampled 24 and 30 h after treatment.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

Amsacrinem-AMSAacridinyl anisidideTopoisomeraseAutophagyInhibitorinhibitorinhibit

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Amsacrine hydrochloride
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