Amrubicin hydrochloride
Based on 1 Customer Validation
Amrubicin (SM-5887) hydrochloride is a DNA topoisomerase II inhibitor, used for the research of cancer.
For research use only. We do not sell to patients.
- Purity: 98.78%
- CAS No.: 110311-30-3
- Formula: C25H26ClNO9
- Molecular Weight:519.93
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Topoisomerase Isoforms
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Biological Activity
|
Topoisomerase II |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.82 μM
Compound: amrubicin hydrochloride
|
Cytotoxicity against human A549 cells after 72 hrs by SRB assay
Cytotoxicity against human A549 cells after 72 hrs by SRB assay
|
[PMID: 17970593] |
| A549 | IC50 |
0.82 μM
Compound: Amrubicin hydrochloride
|
Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay
|
[PMID: 18578539] |
| A549 | IC50 |
0.94 μM
Compound: Amrubicin hydrochloride
|
Cytotoxicity against human A549 cells after 72 hrs by SRB assay
Cytotoxicity against human A549 cells after 72 hrs by SRB assay
|
[PMID: 20681569] |
| HT-29 | IC50 |
4.36 μM
Compound: amrubicin hydrochloride
|
Cytotoxicity against human HT29 cells after 72 hrs by SRB assay
Cytotoxicity against human HT29 cells after 72 hrs by SRB assay
|
[PMID: 17970593] |
| HT-29 | IC50 |
4.36 μM
Compound: Amrubicin hydrochloride
|
Cytotoxicity against human HT29 cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against human HT29 cells after 72 hrs by sulforhodamine B assay
|
[PMID: 18578539] |
| HT-29 | IC50 |
4.57 μM
Compound: Amrubicin hydrochloride
|
Cytotoxicity against human HT-29 cells after 72 hrs by SRB assay
Cytotoxicity against human HT-29 cells after 72 hrs by SRB assay
|
[PMID: 20681569] |
| K562 | IC50 |
1.2 μM
Compound: Amrubicin hydrochloride
|
Cytotoxicity against human K562 cells after 72 hrs by SRB assay
Cytotoxicity against human K562 cells after 72 hrs by SRB assay
|
[PMID: 20681569] |
| K562 | IC50 |
1.26 μM
Compound: amrubicin hydrochloride
|
Cytotoxicity against human K562 cells after 72 hrs by SRB assay
Cytotoxicity against human K562 cells after 72 hrs by SRB assay
|
[PMID: 17970593] |
| K562 | IC50 |
1.26 μM
Compound: Amrubicin hydrochloride
|
Cytotoxicity against human K562 cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against human K562 cells after 72 hrs by sulforhodamine B assay
|
[PMID: 18578539] |
Amrubicin (SM-5887) (2.5 μg/mL) shows radio-enhancement effects on human lung adenocarcinoma A549 cells[1]. Amrubicin (SM-5887) supresses the LX-1, A549, A431, and BT-474 cell lines, with IC50s of 1.1 ± 0.2, 2.4 ± 0.8, 0.61 ± 0.10 and 3.0 ± 0.3 µg/mL, respectively[2]. Amrubicin (SM-5887) inhibits the cell cycle profile of U937 cells with an IC50 of 5.6 µM. Amrubicin (20 µM) also induces apoptosis in U937 cells, activates caspase-3/7 and reduces the mitochondrial membrane potential (Δψm)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 110311-30-3
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Appearance Solid
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Molecular Weight 519.93
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Formula C25H26ClNO9
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Color Brown to red
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SMILES
CC([C@@](C1)(N)C[C@H](O[C@@H]2OC[C@@H](O)[C@@H](O)C2)C(C1=C3O)=C(O)C4=C3C(C5=CC=CC=C5C4=O)=O)=O.Cl
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Synonyms
SM-5887 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
DMSO : ≥ 100 mg/mL (192.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
Aliquots of cells are plated into 96-well microplates. Following cell adherence (1 day), experimental medium either containing or not containing the agents is added to each well. Cells are treated with serial dilutions of each agent individually and with two agents simultaneously at a fixed ratio of doses. After 3 days of incubation with agents at 37°C in 5% CO2, the numbers of viable cells are examined using WST-1 or AlamarBlue. The IC50 value is defined as the concentration inhibiting cell growth by 50% compared with the controls. Multiple drug effects are analyzed by calculating CIs. At least three independent experiments are carried out in triplicate. CI values are calculated based on the conservative assumption of mutually nonexclusive drug interactions. CI values less than and greater than 1 indicate synergism and antagonism, respectively, whereas a value of 1 indicates addition[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Female athymic nude mice, BALB/c nu/nu are injected s.c. with tumor fragments in the flank. A few weeks after this inoculation, mice bearing a tumor approximately 100-300 mm3 in volume are randomLy allocated into different treatment groups and a control group, each of which consisted of six to eight mice. Tumor diameters are serially measured with calipers, and estimated tumor volumes are calculated by the formula: (smaller diameter)3 × (larger diameter)/2. The dosages of the agents tested are as follows: amrubicin (25 mg/kg, i.v.), doxorubicin (12.5 mg/kg, i.v.), cisplatin (10 mg/kg, i.v.), irinotecan (120 mg/kg, i.v.), gemcitabine (300 mg/kg per day, q7d, i.p.), vinorelbine (16 mg/kg, i.p.), trastuzumab (100 mg/kg per day, twice per week × 2 weeks, i.p.), tegafur/uracil (28 mg/kg per day, 5qd, p.o.), and gefitinib (150 mg/kg per day, 5qd, p.o.). In the combination experiments, amrubicin is given approximately 1 h before the other agent on day 0. The tumor growth rate is calculated with the formula: Vn/V0, where Vn is the estimated tumor volume at day n and V0 is the estimated tumor volume at the initiation of the treatment (day 0). The T/C (%) values are calculated by comparing the mean tumor growth rates of the treated group with those of the control group for each day that the tumors are measured. The systemic toxicities of the treatments are assessed in terms of changes in body weight during the experiments. These are calculated as (Wn − W0)/W0 × 100 where Wn is the body weight at day n and W0 is the body weight at the initiation of the treatment (day 0)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (285 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Hayashi S, et al. Enhancement of radiosensitivity by topoisomerase II inhibitor, amrubicin and amrubicinol, in human lung adenocarcinoma A549 cells and kinetics of apoptosis and necrosis induction. Int J Mol Med. 2006 Nov;18(5):909-15. [Content Brief]
[2]. Hanada M, et al. Amrubicin, a novel 9-aminoanthracycline, enhances the antitumor activity of chemotherapeutic agents against human cancer cells in vitro and in vivo. Cancer Sci. 2007 Mar;98(3):447-54. [Content Brief]
[3]. Hanada M, et al. Amrubicin induces apoptosis in human tumor cells mediated by the activation of caspase-3/7 preceding a loss of mitochondrial membrane potential. Cancer Sci. 2006 Dec;97(12):1396-403. Epub 2006 Sep 21. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9233 mL | 9.6167 mL | 19.2334 mL | 48.0834 mL |
| 5 mM | 0.3847 mL | 1.9233 mL | 3.8467 mL | 9.6167 mL | |
| 10 mM | 0.1923 mL | 0.9617 mL | 1.9233 mL | 4.8083 mL | |
| 15 mM | 0.1282 mL | 0.6411 mL | 1.2822 mL | 3.2056 mL | |
| 20 mM | 0.0962 mL | 0.4808 mL | 0.9617 mL | 2.4042 mL | |
| 25 mM | 0.0769 mL | 0.3847 mL | 0.7693 mL | 1.9233 mL | |
| 30 mM | 0.0641 mL | 0.3206 mL | 0.6411 mL | 1.6028 mL | |
| 40 mM | 0.0481 mL | 0.2404 mL | 0.4808 mL | 1.2021 mL | |
| 50 mM | 0.0385 mL | 0.1923 mL | 0.3847 mL | 0.9617 mL | |
| 60 mM | 0.0321 mL | 0.1603 mL | 0.3206 mL | 0.8014 mL | |
| 80 mM | 0.0240 mL | 0.1202 mL | 0.2404 mL | 0.6010 mL | |
| 100 mM | 0.0192 mL | 0.0962 mL | 0.1923 mL | 0.4808 mL |