Bendamustine (SDX105) HCl

For research use only.

Catalog No.S1212 Synonyms: Cytostasane HCl

25 publications

Bendamustine (SDX105) HCl Chemical Structure

CAS No. 3543-75-7

Bendamustine (SDX-105, Cytostasane) HCl is a DNA-damaging agent with IC50 of 50 μM in cell-free assay.

Selleck's Bendamustine (SDX105) HCl has been cited by 25 publications

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Biological Activity

Description Bendamustine (SDX-105, Cytostasane) 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 M{LSenBzd2yrZnXyZZRqd25iYYPzZZk> MVe3NkBp M33RPWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjZoTldkA4OiCqcoOgZpkh[3K7c4ThcEB3cW:uZYSgd5RicW6rbne= M3LyNFIyOzdzN{mw

... 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]
- Collapse
  • 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]
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  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (197.6 mM)
Water 2 mg/mL (5.06 mM)
Ethanol '17 mg/mL
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 Cytostasane HCl
Smiles CN1C2=C(C=C(C=C2)N(CCCl)CCCl)N=C1CCCC(=O)O.Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05023980 Not yet recruiting Drug: Pirtobrutinib|Drug: Bendamustine|Drug: Rituximab Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma Loxo Oncology Inc.|Eli Lilly and Company September 2021 Phase 3
NCT03406156 Active not recruiting Drug: Obinutuzumab|Drug: Bendamustine|Drug: Venetoclax Chronic Lymphocytic Leukemia (CLL)|Small Lymphocytic Lymphoma (SLL) AbbVie August 10 2018 Phase 3
NCT03604679 Completed Drug: SyB C-0501 Advanced Solid Tumor SymBio Pharmaceuticals May 24 2018 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID