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Purity: ≥98%
Bendamustine HCl (formerly also called SDX-105; EP-3101; Cytostasane; DD6304600; Treanda), the hydrochloride salt of bendamustine which is a bifunctional mechlorethamine derivative, is a potent DNA-alkylating/ cross-linking / damaging agent (IC50 = 50 μM in cell-free assay) approved for cancer treatment. It has been documented that apoptosis and DNA damage stress activate bendamustine. By suppressing a number of genes linked to mitosis, including Cyclin B1, Aurora kinase A, and Polo-like kinase 1, bendamustine prevents mitotic checkpoints and causes a mitotic catastrophe. Bendamustine caused G2 cell cycle arrest in myeloma cell lines by cleaving caspase 3, which triggered apoptosis.
| Targets |
DNA Alkylator/Crosslinker
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| Cell Assay |
Bendamustine and melphalan both exhibit cytotoxicity on multiple myeloma (MM) cells, which is quantified as an inhibition of cell viability based on the MTS assay's percentage of cell survival. In summary, 96-well plates are seeded with 1 × 104 cells per well, and the drug is added in increasing concentrations. The cells are then incubated for 24, 48, 72, and 96 hours before analysis. In order to achieve this, 1 μg/mL of MTS solution is added to each well. The dark blue formazan crystals are then dissolved by isopropanol 1 N and HCl (24:1, vol/vol) after 1 hour at 37 °C. Ultimately, a 96-well plate reader is used to measure the absorbance at 490 nm. For each test, triplicates are used, and the percentage of untreated control absorbance is used to estimate cell survival. Bendamustine and melphalan equitoxic concentrations are used for parallel testing. The inhibitory concentrations 50 (IC50) and 25 (IC25) of each drug are determined, which represent the amounts able to reduce cell growth to 50% and 25%, respectively, of that of untreated control cells. By dividing the IC50 of 8226-LR5 by the IC50 of RPMI-8226 cells, one can calculate the relative resistance index (RRI).
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Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation No information is available on the use of bendamustine during breastfeeding. Most sources consider breastfeeding to be contraindicated during maternal antineoplastic drug therapy, especially alkylating agents such as bendamustine. Based on the half-life of the drug and its metabolites, the drug should be eliminated from the milk by 24 to 48 hours after the last dose. The manufacturer recommends that breastfeeding be discontinued during bendamustine therapy and for at least 1 week after the last dose. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Some evidence indicates that the closely related drug carmustine can increase serum prolactin. |
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| Additional Infomation |
Bendamustine Hydrochloride is the hydrochloride salt of bendamustine, a bifunctional mechlorethamine derivative with alkylator and antimetabolite activities. Bendamustine possesses three active moieties: an alkylating group; a benzimidazole ring, which may act as a purine analogue; and a butyric acid side chain. Although its exact mechanism of action is unknown this agent appears to act primarily as an alkylator. Bendamustine metabolites alkylate and crosslink macromolecules, resulting in DNA, RNA and protein synthesis inhibition, and, subsequently, apoptosis. Bendamustine may differ from other alkylators in that it may be more potent in activating p53-dependent stress pathways and inducing apoptosis; it may induce mitotic catastrophe; and it may activate a base excision DNA repair pathway rather than an alkyltransferase DNA repair mechanism. Accordingly, this agent may be more efficacious and less susceptible to drug resistance than other alkylators.
A nitrogen mustard compound that functions as an ALKYLATING ANTINEOPLASTIC AGENT and is used in the treatment of CHRONIC LYMPHOCYTIC LEUKEMIA and NON-HODGKIN'S LYMPHOMA. See also: Bendamustine (has active moiety). |
| Molecular Formula |
C16H21CL2N3O2.HCL
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| Molecular Weight |
394.72
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| Exact Mass |
393.077
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| Elemental Analysis |
C, 48.68; H, 5.62; Cl, 26.95; N, 10.65; O, 8.11
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| CAS # |
3543-75-7
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| Related CAS # |
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| PubChem CID |
77082
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| Appearance |
Solid powder
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| Melting Point |
149-151°C
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| LogP |
4.066
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
24
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| Complexity |
380
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC([H])([H])C([H])([H])N(C([H])([H])C([H])([H])Cl)C1C([H])=C([H])C2=C(C=1[H])N=C(C([H])([H])C([H])([H])C([H])([H])C(=O)O[H])N2C([H])([H])[H].Cl[H]
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| InChi Key |
ZHSKUOZOLHMKEA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H21Cl2N3O2.ClH/c1-20-14-6-5-12(21(9-7-17)10-8-18)11-13(14)19-15(20)3-2-4-16(22)23;/h5-6,11H,2-4,7-10H2,1H3,(H,22,23);1H
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| Chemical Name |
4-[5-[bis(2-chloroethyl)amino]-1-methylbenzimidazol-2-yl]butanoic acid;hydrochloride
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| Synonyms |
SDX-105 (Cytostasane) HCl; EP-3101; SDX105; EP 3101; SDX 105; SDX-105; EP3101; DD6304600; Bendamustinum; Bendamustina; Ribomustin. Brand name: Treanda.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1% DMSO +30% polyethylene glycol+1% Tween 80 : 30 mg/mL Solubility in Formulation 5: 5.88 mg/mL (14.90 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5334 mL | 12.6672 mL | 25.3344 mL | |
| 5 mM | 0.5067 mL | 2.5334 mL | 5.0669 mL | |
| 10 mM | 0.2533 mL | 1.2667 mL | 2.5334 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02996773 | Active Recruiting |
Drug: Bendamustine Drug: Cyclophosphamide |
Lymphoma, Hodgkin Lymphoma, Follicular |
University of Arizona | November 29, 2016 | Phase 1 |
| NCT03834688 | Active Recruiting |
Drug: Bendamustinee Drug: Venetoclax |
Mantle Cell Lymphoma | PrECOG, LLC. | January 13, 2020 | Phase 2 |
| NCT04083898 | Active Recruiting |
Drug: Bendamustine Drug: Prednisone |
Multiple Myeloma | Washington University School of Medicine |
April 3, 2020 | Phase 1 |
| NCT03872180 | Active Recruiting |
Drug: Bendamustine Biological: Obinutuzumab |
CCND1 Positive Mantle Cell Lymphoma |
Emory University | April 11, 2019 | Phase 2 |
| NCT03311126 | Active Recruiting |
Drug: Bendamustine Drug: Obinutuzumab |
Mantle Cell Lymphoma Non-hodgkin Lymphoma |
University of Wisconsin, Madison | October 19, 2017 | Phase 2 |
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