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Purity: ≥98%
Carmustine (Nitrumon; NSC 409962), an DNA crosslinking and alkylating nitrosourea, is a potent antitumor chemotherapeutic agent. Carmustine disrupts DNA function, causes cell cycle arrest, and induces apoptosis by alkylating and cross-linking DNA at every stage of the cell cycle. Moreover, this substance carbamoylates proteins, including enzymes that repair DNA, which increases its cytotoxic effect. Since carmustine is so lipophilic, it easily penetrates the blood-brain barrier.
| Targets |
DNA Alkylator
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|---|---|
| ln Vitro |
Carmustine is a chemotherapy drug used to treat cancer. Neuronal cell proliferation, tumor cytoplasm, and intact N-benzoyltransferase (NAT) activity of 2-aminobenzoic acid (AF) and p-aminobenzoic acid (PABA) are all reduced by carmustine (8, 80, and 800 μM). The DNA-AF addition complex rises with the development of tumor nerve growth cells, while carmustine lowers it [1].
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| ln Vivo |
In comparison to stents level (GSSG) and reduced glutathione (GSH)/GSSG value, carmustine (BCNU; 25 mg/kg, ip) led to greater levels of death to body weight, the ratio of bound bilirubin, external bile flow, and oxidized glutathione [2].
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| Enzyme Assay |
2-Aminofluorene (AF) and p-Aminobenzoic acid (PABA) N-acetylation is determined in an Acetyl-CoAdependent manner. The assay system's incubation mixtures have a total volume of 90 μL and include glial tumor cells cytosols, diluted as needed, in 50 μL of lysis buffer (20 mM Tris/HCl, pH 7.5, 1 mM DTT and 1 mM EDTA), 20 μL of an Acetyl-CoA recycling mixture of 50 mM Tris-HCl (pH7.5), 0.2 mM EDTA, 2 mM DTT, 15 mM acetylcamitine, 2U/mL carnitine acetyltransferase, and AF or PABA at designated concentrations. Addition of 20 μL of acetyl-CoA initiates the reactions. Acetyl-CoA is replaced in the control reactions with 20 μL of distilled water. The final concentrations of AcCoA and PABA for the single point activity measurements are 0.5 mM and 0.1 mM, respectively. 50 μL of 20% trichloroacetic acid is used to stop the PABA reactions and 100 μL of acetonitrile is used to stop the AF reactions after the reaction mixtures, either with or without specific concentrations of carmustine and lomustine, are incubated for 10 minutes at 37°C. Every reaction, including controls and experiments, is carried out in triplicate[1].
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| Animal Protocol |
Rats: Rats are randomly assigned to four groups after being weighted individually before beginning the study and having their weights recorded. There are twelve rats in Group I (the saline group). The study includes the rats 48 hours after they receive an intraperitoneal (IP) injection of 2 mL/kg of saline 48 hours prior to the study. Fifteen rats make up Group II (corn oil group). The rats receive a 2 mL/kg injection of corn oil (vehicle) IP 48 hours prior to the investigation. Sixteen rats make up Group III (Carmustine group). For three days, the same hour of the day, a single-dose of 1 mL of saline IP is injected into these rats. The rats are added to the study 48 hours after the first dose of saline is administered, and twelve hours later, they receive injections of corn oil (2 mL/kg) and carmustine (25 mg/kg IP). There are twelve rats in Group IV (the trimetazidine group). For three days, these rats receive a single-dose injection of 2.5 mg/kg of trimetazidine (TMZ) IP at the same hour every day. Corn oil (2 mL/kg) and carmustine (25 mg/kg IP) are injected 12 hours after the first dose of TMZ, and the rats are added to the study 48 hours later[2].
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| References |
[1]. Hung CF. Effects of carmustine and lomustine on arylamine N-acetyltransferase activity and 2-aminofluorene-DNA adducts in rat glial tumor cells. Neurochem Res. 2000 Jun;25(6):845-51.
[2]. Demir A, et al. The effect of trimetazidine on intrahepatic cholestasis caused by carmustine in rats. Hepatol Res. 2001 May 1;20(1):133-143 |
| Molecular Formula |
C5H9CL2N3O2
|
|---|---|
| Molecular Weight |
214.0499
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| Exact Mass |
213.01
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| Elemental Analysis |
C, 28.06; H, 4.24; Cl, 33.12; N, 19.63; O, 14.95
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| CAS # |
154-93-8
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| Related CAS # |
Carmustine-d8
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| Appearance |
Light yellow solid (low temperature)
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| SMILES |
C(CCl)NC(=O)N(CCCl)N=O
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| InChi Key |
DLGOEMSEDOSKAD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H9Cl2N3O2/c6-1-3-8-5(11)10(9-12)4-2-7/h1-4H2,(H,8,11)
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| Chemical Name |
1,3-bis(2-chloroethyl)-1-nitrosourea
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| Synonyms |
NSC409962; NCI-C04773; NCIC04773; NCI C04773; Nitrumon; NSC 409962; NSC-409962; SK 27702; SRI 1720; DTI 015;; FDA 0345; BCNU Becenum; Bi CNU; BiCNU; Carmustine
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| HS Tariff Code |
29241900
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO: ≥ 35 mg/mL (~163.5 mM)
H2O: ~100 mg/mL (~467.2 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (9.72 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 (9.72 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 (9.72 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: 5%DMSO+ 40%PEG300+ 5%Tween 80+ 50%ddH2O: 2.0mg/ml (9.34mM) Solubility in Formulation 5: 100 mg/mL (467.18 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6718 mL | 23.3590 mL | 46.7181 mL | |
| 5 mM | 0.9344 mL | 4.6718 mL | 9.3436 mL | |
| 10 mM | 0.4672 mL | 2.3359 mL | 4.6718 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 |
| NCT02443077 | Active Recruiting |
Drug: Carmustine Drug: Cytarabine |
Recurrent Diffuse Large B-Cell Lymphoma Activated B-Cell Type |
National Cancer Institute (NCI) |
October 12, 2016 | Phase 3 |
| NCT02797470 | Active Recruiting |
Drug: Carmustine Drug: Cytarabine |
HIV Infection Plasmablastic Lymphoma |
AIDS Malignancy Consortium | June 23, 2016 | Phase 1 Phase 2 |
| NCT02342782 | Active Recruiting |
Drug: Carmustine Drug: Etoposide |
Mature T-Cell and NK-Cell Non-Hodgkin Lymphoma |
City of Hope Medical Center | June 8, 2020 | Phase 1 |
| NCT01476839 | Active Recruiting |
Drug: carmustine Drug: etoposide |
Recurrent Adult Hodgkin Lymphoma |
City of Hope Medical Center | November 9, 2012 | Phase 1 |
| NCT00641381 | Active Recruiting |
Drug: carmustine Drug: cyclophosphamide |
Lymphoma | City of Hope Medical Center | May 10, 2000 | Phase 1 |
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