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Bendamustine HCl

Bendamustine HCl

Item no.	S1212-1000
Manufacturer	Selleckchem
CASRN	3543-75-7
Amount	1 g
Quantity options	100 mg 1 g 10 g 10 mM/1 ml 25 mg 5 mg 50 mg 5 g
Category	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Skin Cancer Breast Cancer Lymphatic System Cancer Uterine, Ovarian & Cervical Cancer
Type	Inhibitors
Specific against	other
Smiles	CN1C2=C(C=C(C=C2)N(CCCl)CCCl)N=C1CCCC(=O)O.Cl
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	SDX105 HCl,Cytostasane HCl
Similar products	Bendamustine
Available
Storage Conditions	2 years -80 in solvent
Molecular Weight	394, 72
Administration	Administered via i.v.
Animal Models	C.B.-17 scid mice bearing DoHH-2, Granta 519 or C.B.-17 scid-bg mice bearing SuDHL-4, RAMOS
Cell lines	SU-DHL-1 and SU-DHL-9 cells
Clinical Trials	Bendamustine HCl has entered in a phase II clinical trial in the treatment of ovarian cancer.
Concentrations	0-100 uM
Dosages	25 mg/kg
Formulation	Control
IC50	50 uM [1], 50 uM [1], 50 uM [1], 50 uM [1], 50 uM [1], 50 uM [1]
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 nonâ€“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 ug/mL to 50 ug/mL, a dose- and time-dependent manner of cytotoxicity from 30.4% to 94.8% after 48 hours could be observed. e LD50 for untreated and pretreated CLL cells is 7.3 or 4.4 ug /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]
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 uM 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.
Solubility (25C)	DMSO 79 mg/mL, Water 15 mg/mL, Ethanol 17 mg/mL
Information	Bendamustine HCl is a DNA-damaging agent with IC50 of 50 μM in cell-free assay.

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S1212-1000-datasheet.pdf

S1212-1000-safety-datasheet.pdf