Home DNA Damage/DNA Repair DNA/RNA Synthesis chemical Bendamustine HCl For research use only.

Bendamustine HCl

Synonyms: SDX105 HCl, Cytostasane HCl

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

Bendamustine HCl Chemical Structure

Bendamustine HCl Chemical Structure

CAS No. 3543-75-7

Purity & Quality Control

Bendamustine HCl Related Products

Signaling Pathway

DNA/RNA Synthesis Signaling Pathways

DNA/RNA Synthesis Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MDA-MB-231 cells Proliferation assay 72 h Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by crystal violet staining 21371790
Click to View More Cell Line Experimental Data

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
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 Research 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.
In Vivo
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]
Animal Research Animal Models C.B.-17 scid mice bearing DoHH-2, Granta 519 or C.B.-17 scid-bg mice bearing SuDHL-4, RAMOS
Dosages 25 mg/kg
Administration Administered via i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05551936 Recruiting
Follicular Lymphoma
Vaishalee Kenkre|Epizyme Inc.|University of Wisconsin Madison|Big Ten Cancer Research Consortium
 January 26 2023 Phase 1|Phase 2
NCT05023980 Active not recruiting
Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma
Loxo Oncology Inc.|Eli Lilly and Company
 September 23 2021 Phase 3

Chemical Information & Solubility

Molecular Weight 394.72 Formula

C16H21Cl2N3O2.HCl
CAS No. 3543-75-7 SDF Download Bendamustine HCl SDF
Smiles CN1C2=C(C=C(C=C2)N(CCCl)CCCl)N=C1CCCC(=O)O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 79 mg/mL ( (200.14 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 79 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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