Bisantrene
Based on 6 publication(s) in Google Scholar
Bisantrene is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene targets eukaryotic type II topoisomerases. Bisantrene is a substrate of MDR1.
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- 純度: 98.06%
- CAS 番号: 78186-34-2
- 分子式: C22H22N8
- 分子量:398.46
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Bisantrene
MoreTopoisomerase アイソフォーム固有の製品をすべて表示
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生物活性
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Topoisomerase II |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
0.34 μM
Compound: Bisantrene
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Cell cytotoxicity was determined against human ovarian cancer (A2780) cell line
Cell cytotoxicity was determined against human ovarian cancer (A2780) cell line
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[PMID: 9871638] |
| A549 | IC50 |
0.017 μM
Compound: 1
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Compound was tested for potency against human lung A549 cells using sulforhodamine B assay.
Compound was tested for potency against human lung A549 cells using sulforhodamine B assay.
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[PMID: 9371238] |
| HL-60 | IC50 |
0.3 μM
Compound: Bisantrene
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Cell cytotoxicity was determined against human promyelocytic leukemia (HL60) cell line
Cell cytotoxicity was determined against human promyelocytic leukemia (HL60) cell line
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[PMID: 9871638] |
| L1210 | IC50 |
0.049 μM
Compound: 1
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Compound was tested for potency against multidrug-resistant murine leukemia L1210 cells
Compound was tested for potency against multidrug-resistant murine leukemia L1210 cells
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[PMID: 9371238] |
| L1210 | IC50 |
3.2 μM
Compound: 1
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Compound was tested for potency against multi drug resistant murine leukemia L1210 cells.
Compound was tested for potency against multi drug resistant murine leukemia L1210 cells.
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[PMID: 9371238] |
| OCI-AML2 | IC50 |
100 nM
Compound: 39; CS1
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Antiproliferative activity against human OCI-AML2 cells assessed as reduction in cell viability
Antiproliferative activity against human OCI-AML2 cells assessed as reduction in cell viability
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[PMID: 38805939] |
| RPMI-8226 | IC50 |
0.018 μM
Compound: 1
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Compound was tested for potency against human myeloma 8226 cells using MTT assay method.
Compound was tested for potency against human myeloma 8226 cells using MTT assay method.
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[PMID: 9371238] |
| RPMI-8226 | IC50 |
9.1 μM
Compound: 1
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Compound was tested for potency against human myeloma 8226 cells (40 fold resistant to doxorubicin).
Compound was tested for potency against human myeloma 8226 cells (40 fold resistant to doxorubicin).
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[PMID: 9371238] |
| SW480 | IC50 |
0.09 μM
Compound: 1
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Compound was tested for potency against human colon carcinoma SW 480 cells in a sulforhodamine B assay.
Compound was tested for potency against human colon carcinoma SW 480 cells in a sulforhodamine B assay.
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[PMID: 9371238] |
| WiDr | IC50 |
0.79 μM
Compound: 1
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Compound was tested for potency against human colon carcinoma WiDr cells in a sulforhodamine B assay.
Compound was tested for potency against human colon carcinoma WiDr cells in a sulforhodamine B assay.
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[PMID: 9371238] |
Bisantrene promots DNase I cleavage at oligopurine-oligopyrimidine tracts and slightly reduces the cleavage activity at alternating purine-pyrimidine sequences[1].? Bisantrene is an inhibitor of [3H]uridine incorporation into RNA and [3H]thymidine incorporation into DNA[2].
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
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 78186-34-2
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性状 Solid
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分子量 398.46
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分子式 C22H22N8
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Color Orange to red
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SMILES
C12=CC=CC=C1C(/C=N/NC3=NCCN3)=C4C(C=CC=C4)=C2/C=N/NC5=NCCN5
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別名
CL216942
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Mol Cancer
AI-based classification of anticancer drugs reveals nucleolar condensation as a predictor of immunogenicity. [Abstract]2024 Dec 20;23(1):275. PMID: 39702289 -
Nat Commun
Autophagy of the m6A mRNA demethylase FTO is impaired by low-level arsenic exposure to promote tumorigenesis. [Abstract]2021 Apr 12;12(1):2183. PMID: 33846348 -
Mol Cell
R-2-hydroxyglutarate attenuates aerobic glycolysis in leukemia by targeting the FTO/m6A/PFKP/LDHB axis. [Abstract]2021 Mar 4;81(5):922-939.e9. PMID: 33434505 -
Anal Chem
Metal-Enhanced Aggregation-Induced Emission Strategy for the HIV-I RNA-Binding Ligand Assay. [Abstract]2022 Mar 22;94(11):4695-4702. PMID: 35258935 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
溶剤 & 溶解度
DMSO : 1 mg/mL (2.51 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
Measurements are carried out at 25°C in ETN buffer (1 mM EDTA, 10 mM Tris, pH 7.0, with NaCl to obtain the desired ionic strength). Binding is monitored spectrophotometrically or fluorometrically, in the ligand absorption or emission region, respectively, after addition of scalar amounts of DNA to a freshly prepared drug solution. To avoid large systematic inaccuracies resulting from experimental errors in extinction coefficients or fluorescence quantum yield, the range of bound drug fractions is 0.15-0.85. Data are evaluated. Spectroscopic measurements are made with a Perkin-Elmer Lambda 5 apparatus and a MPF66 fluorometer, both equipped with a Haake F3-C thermostat[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (278 KB)
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SDS (537 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Sissi C, et al. DNA-binding preferences of Bisantrene analogues: relevance to the sequence specificity of drug-mediated topoisomerase II poisoning. Mol Pharmacol. 1998 Dec;54(6):1036-45. [Content Brief]
[2]. Yap HY, et al. Bisantrene, an active new drug in the treatment of metastatic breast cancer. Cancer Res. 1983 Mar;43(3):1402-4. [Content Brief]
[3]. Wang BS, et al. Activation of tumor-cytostatic macrophages with the antitumor agent 9,10-anthracenedicarboxaldehyde bis[(4,5-dihydro-1H-imidazole-2-yl)hydrazone] dihydrochloride (bisantrene). Cancer Res. 1984 Jun;44(6):2363-7. [Content Brief]
[4]. Aksentijevich I, et al. Retroviral transfer of the human MDR1 gene confers resistance to bisantrene-specific hematotoxicity. Clin Cancer Res. 1996 Jun;2(6):973-80. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5097 mL | 12.5483 mL | 25.0966 mL | 62.7416 mL |
Bisantrene 関連分類
HY-100875 関連分類
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