Bendamustine HCl

Catalog No.S1212 Synonyms: SDX-105 (Cytostasane) HCl

Bendamustine HCl Chemical Structure

Molecular Weight(MW): 394.72

Bendamustine HCL is a DNA-damaging agent with IC50 of 50 μM in cell-free assay.

Size Price Stock Quantity  
In DMSO USD 420 In stock
USD 70 In stock
USD 210 In stock
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3 Customer Reviews

  • Cells were grown for 6-8 days in presence of increasing concentrations of (I) bendamustine. Relative toxicity of the drugs was determined by the WST-8 cell proliferation assay, Dashed lines with open circles or triangles indicate cell proliferation in absence of an anti-lymphoma drug. Other curves represent the cells grown in increasing concentrations (indicated by the associated number) of the tested drug. Maximal absorbance (highest number of viable cells) of cells grown without an anti-lymphoma agent in each experiment was set as 100%. Standard deviations were < 5% for all measurements.

    PLoS One, 2015, 10(8):e0135314.. Bendamustine HCl purchased from Selleck.

    Fractional Analysis of Combination Therapy of SGI-1776 With Bendamustine in B-Cell Lymphoma.

    Clin Lymphoma Myeloma Leuk 2013 13 Suppl 2, S355-62. Bendamustine HCl purchased from Selleck.

  • Inhibition of DNA Synthesis by SGI-1776 (S) and Bendamustine (B) and Their Combination in JeKo-1 Cells. JeKo-1 Cells Were Treated With Dimethyl Sulfoxide (DMSO), 5 μM or 10 m M Bendamustine, 5 μM SGI-1776, or 5 μM or 10 m M Bendamustine Combined With 5 μM SGI-1776 for 24 Hours. Cells were Then Incubated With [Methyl-3H]-Thymidine at 0.8 m Ci/mL Concentration for 45 Minutes. Radioactive Incorporation Was Then Measured by Scintillation Count, and Values Were Recorded as Disintegration per Minute per Cell and Normalized to DMSO Controls. Experiments Were Performed in Triplicate and Presented as Mean ± Standard Error of the Mean.

    Clin Lymphoma Myeloma Leuk 2013 13 Suppl 2, S355-62. Bendamustine HCl purchased from Selleck.

Purity & Quality Control

Choose Selective DNA/RNA Synthesis Inhibitors

Biological Activity

Description Bendamustine HCL is a DNA-damaging agent with IC50 of 50 μM in cell-free assay.
Targets
DNA synthesis [1]
(Cell-free assay)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MDA-MB-231 cells NF[ySnlRem:uaX\ldoF1cW:wIHHzd4F6 MXm3NkBp NV6ydJM1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSClconzeIFtKH[rb3zleEB{fGGrbnnu[y=> MX:yNVM4OTd7MB?=

... Click to View More Cell Line Experimental Data

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]

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: SU-DHL-1 and SU-DHL-9 cells
  • Concentrations: 0-100 μM
  • Incubation Time: 72 hours
  • Method: 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.
    (Only for Reference)
Animal Research:[5]
+ Expand
  • Animal Models: C.B.-17 scid mice bearing DoHH-2, Granta 519 or C.B.-17 scid-bg mice bearing SuDHL-4, RAMOS
  • Formulation: Control
  • Dosages: 25 mg/kg
  • Administration: Administered via i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (197.6 mM)
Ethanol 17 mg/mL (43.06 mM)
Water 2 mg/mL (5.06 mM)
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
30 mg/mL

* 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.

Chemical Information

Molecular Weight 394.72
Formula

C16H21Cl2N3O2.HCl

CAS No. 3543-75-7
Storage powder
in solvent
Synonyms SDX-105 (Cytostasane) HCl

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02477215 Active not recruiting Multiple Myeloma Parameswaran Hari|Medical College of Wisconsin October 9 2015 Phase 1|Phase 2
NCT02008006 Recruiting Follicular Lymphoma Centre Leon Berard July 9 2014 Phase 2
NCT02071225 Active not recruiting Chronic Lymphocytic Leukemia Hoffmann-La Roche April 9 2014 Phase 2
NCT01886872 Active not recruiting CD19 Positive|CD20 Positive|CD5 Positive|Stage I Chronic Lymphocytic Leukemia|Stage II Chronic Lymphocytic Leukemia|Stage III Chronic Lymphocytic Leukemia|Stage IV Chronic Lymphocytic Leukemia National Cancer Institute (NCI) December 9 2013 Phase 3
NCT01891227 Completed Breast Cancer Arbeitsgemeinschaft medikamentoese Tumortherapie August 9 2013 Phase 2
NCT01535924 Active not recruiting Adult Lymphocyte Depletion Hodgkin Lymphoma|Adult Lymphocyte Predominant Hodgkin Lymphoma|Adult Mixed Cellularity Hodgkin Lymphoma|Adult Nodular Lymphocyte Predominant Hodgkin Lymphoma|Adult Nodular Sclerosis Hodgkin Lymphoma|Recurrent Adult Hodgkin Lymphoma Beth Christian|Ohio State University Comprehensive Cancer Center February 9 2012 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID