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Cat.No.S1212
| Related Targets | HDAC PARP ATM/ATR DNA-PK WRN Topoisomerase PPAR Sirtuin Casein Kinase eIF |
|---|---|
| Other DNA/RNA Synthesis Inhibitors | B02 CX-5461 (Pidnarulex) SCR7 EED226 Favipiravir (T-705) RK-33 Carmofur Triapine (3-AP) BMH-21 YK-4-279 |
| 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 | |||
| Click to View More Cell Line Experimental Data | ||||||
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In vitro |
DMSO
: 79 mg/mL
(200.14 mM)
Ethanol : 79 mg/mL Water : Insoluble |
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In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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Working concentration: mg/ml;
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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| Molecular Weight | 394.72 | Formula | C16H21Cl2N3O2.HCl |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 3543-75-7 | Download SDF | Storage of Stock Solutions |
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| Synonyms | SDX105 HCl, Cytostasane HCl | Smiles | CN1C2=C(C=C(C=C2)N(CCCl)CCCl)N=C1CCCC(=O)O.Cl | ||
| Targets/IC50/Ki |
DNA synthesis
(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. 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. 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.
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| 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).
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| 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 |
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