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化学情報
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Synonyms | SDX105 HCl, Cytostasane HCl | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C16H21Cl2N3O2.HCl |
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| 分子量 | 394.72 | CAS No. | 3543-75-7 | |
| Solubility (25°C)* | 体外 | DMSO | 78 mg/mL (197.6 mM) | |
| Ethanol | 17 mg/mL (43.06 mM) | |||
| Water | 2 mg/mL (5.06 mM) | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | Bendamustine HCl is a DNA-damaging agent with IC50 of 50 μM in cell-free assay. |
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| in vitro | DNA single- and double-strand breaks caused by Bendamustine are more extensive and significantly more durable than those caused by cyclophosphamide, cisplatinum, or carmustine. Bendamustine specifically regulates, transcriptionally and posttranslationally, genes involved in apoptosis, DNA repair, and mitotic checkpoints. Bendamustine uniquely regulates DNA repair pathways in non–Hodgkin's lymphoma cells compared with other alkylators. Bendamustine inhibits mitotic checkpoints and induces mitotic catastrophe. Treatment with Bendamustine results in a 60% to 80% down-regulation of the mRNA expression of all three of these genes [polo-like kinase 1 (PLK-1), Aurora Kinase A, and cyclin B1] in SU-DHL-9 cells. Twenty-six percent of the Bendamustine-treated MCF-7/ADR cells showed micronucleation compared with only 6% in DMSO control cells. [1] Using Bendamustine alone in concentrations from 1 μg/mL to 50 μg/mL, a dose- and time-dependent manner of cytotoxicity from 30.4% to 94.8% after 48 hours could be observed. The LD50 for untreated and pretreated CLL cells is 7.3 or 4.4 μg /mL, respectively. [2] Myeloid and breast carcinoma cell lines are resistant towards Bendamustine with the exception of HL-60 cells which exhibit an intermediate sensitivity. Bendamustine is found to have a very low clastogenic effect as compared with equimolar doses of lomustine. [3] |
| in vivo | A single dose of Bendamustine at 25 mg/kg demonstrates significant activity in all three tumor lines (DoHH-2, Granta 519 and RAMOS). DoHH-2 is the most sensitive, with 30% ORR and a 69% inhibition in tumor growth. Growth of Granta 519 and RAMOS is also inhibited by Bendamustine (%TGI of 74% and 81%, respectively), and the effect is more durable in Granta 519 (%TGD of 124%) than for DoHH-2 or RAMOS (69% and 43%, respectively). [4] |
プロトコル(参考用のみ)
| 細胞アッセイ | 細胞株 | SU-DHL-1 and SU-DHL-9 cells |
|---|---|---|
| 濃度 | 0-100 μM | |
| 反応時間 | 72 hours | |
| 実験の流れ | SU-DHL-1 and SU-DHL-9 cells are preincubated for 30 minutes with either 6 mM methoxyamine or 50 μM O6-benzylguanine, inhibitors of Ape-1 base excision repair enzyme, or alkylguanyl transferase enzyme, respectively. The cells are then exposed to various concentrations of Bendamustine for 72 hours. Cytotoxicity is evaluated by the MTT viability assay and an IC50 is determined as the drug concentration that inhibited by 50% the viability value of the untreated control. Analyses are done. | |
| 動物実験 | 動物モデル | C.B.-17 scid mice bearing DoHH-2, Granta 519 or C.B.-17 scid-bg mice bearing SuDHL-4, RAMOS |
| 投薬量 | 25 mg/kg | |
| 投与方法 | Administered via i.v. |
参考
カスタマーフィードバック
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Data from [Data independently produced by Clin Lymphoma Myeloma Leuk, 2013, 13 Suppl 2, S355-62]
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Data from [Data independently produced by Clin Lymphoma Myeloma Leuk, 2013, 13 Suppl 2, S355-62]
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Data from [Data independently produced by , , Apoptosis, 2017, 22(6):827-840]
Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| Comparable Efficacy of Oral Bendamustine versus Intravenous Administration in Treating Hematologic Malignancies [ Res Sq, 2024, rs.3.rs-3848777] | PubMed: 38313301 |
| PGD2 displays distinct effects in diffuse large B-cell lymphoma depending on different concentrations [ Cell Death Discov, 2023, 9(1):39] | PubMed: 36725845 |
| Partially replacing cyclophosphamide with bendamustine in combination with cyclosporine A improves survival and reduces xenogeneic graft-versus-host-disease [ Front Immunol, 2022, 13:1045710] | PubMed: 36700195 |
| Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] | PubMed: 35207746 |
| Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y] | PubMed: 35118583 |
| HAPLN1 confers multiple myeloma cell resistance to several classes of therapeutic drugs [ PLoS One, 2022, 17(12:e0274704)] | PubMed: 36480501 |
| Brentuxinmab vedotin, alone or combine with bendamustine in the treatment of natural killer T cell lymphoma [ Hematol Oncol, 2022, 10.1002/hon.3042] | PubMed: 35797410 |
| The potential efficacy and mechanism of bendamustine in entra-nodal NK/T cell lymphoma [ Hematol Oncol, 2022, 10.1002/hon.3007] | PubMed: 35439335 |
| Resistance to obinutuzumab-induced antibody-dependent cellular cytotoxicity caused by abnormal Fas signaling is overcome by combination therapies [ Mol Biol Rep, 2022, 49(6):4421-4433] | PubMed: 35218445 |
| Resistomes and microbiome of meat trimmings and colon content from culled cows raised in conventional and organic production systems [ Anim Microbiome, 2022, 4(1):21] | PubMed: 35272712 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。