Bendamustine HCl

Catalog No.S1212 Batch:S121206

Technical Data

Formula	C₁₆H₂₁Cl₂N₃O₂.HCl
Molecular Weight	394.72	CAS No.	3543-75-7
Solubility (25°C)*	In vitro	DMSO	78 mg/mL (197.6 mM)
		Ethanol	78 mg/mL (197.6 mM)
		Water	13 mg/mL (32.93 mM)
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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]

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 (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[5]}	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.

Cell Assay:^{^[1]}

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.

Animal Study:^{^[5]}

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.

References

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Customer Product Validation

: Data from [Data independently produced by Clin Lymphoma Myeloma Leuk, 2013, 13 Suppl 2, S355-62]

: Data from [Data independently produced by Clin Lymphoma Myeloma Leuk, 2013, 13 Suppl 2, S355-62]

: Data from [Data independently produced by , , Apoptosis, 2017, 22(6):827-840]

: Data from [Data independently produced by , , PLoS One, 2015, 10(8):e0135314.]

Selleck's Bendamustine HCl has been cited by 35 publications

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
Glycoprotein PTGDS promotes tumorigenesis of diffuse large B-cell lymphoma by MYH9-mediated regulation of Wnt-β-catenin-STAT3 signaling [ Cell Death Differ, 2021, 10.1038/s41418-021-00880-2]	PubMed: 34743203

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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