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Purity: ≥98%
Chlorambucil (CB-1348; WR-139013; CB 1348; WR 139013; chloraminophen; Chlorbutin; chlorbutine; chlorbutinum; Leukersan; Leukoran) is an approved antitumor medication mainly used in the treatment of chronic lymphocytic leukemia. It functions as an oral-active nitrogen mustard alkylating agent by cross-linking and alkylating DNA at every stage of the cell cycle, which causes apoptosis, cell cycle arrest, and disruption of DNA function.
| Targets |
DNA Alkylator
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|---|---|
| ln Vitro |
By enhancing the complementary chain of DNA molecules, chlorambucil inhibits the growth of tumor cells by causing an alkalinization-induced cross-reaction. Chlorambucil (0, 2.5, 5, 10 μM) significantly enhanced the expression of DR4 and DR5 mRNA in Raji cells while having a minor blocking impact on them. Rati cells treated with 10 μM chlorambucil and 80 ng/mL of tumor factor-related phosphate ligand (TRAIL) expressed DR4 and DR5 mRNA. Chlorambucil is a DNA alkylating agent at high concentrations and a ligand for nuclear protein synthesis, particularly proteome production, at low concentrations. While long-term treatment maintenance is linked to p53 gene alterations that cause subsequent cancers, increasing doses are linked to a higher frequency of cell sterilization [4].
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| ln Vivo |
Ehrlich ascites cancer can be treated with levamisole (5 mg/kg) and chlorambucil (0.2 mg/kg, po) in combination to increase the anti-cancer effect and improve the transparency and anti-cancer rate of the disease. Mice's kidneys and liver are negatively impacted by it [2].
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| Cell Assay |
After being broken down by trypsin into a single cell suspension, cultured cells at the log-growth phase are seeded at a density of 1000 cells per well into 96-well plates. The plate is set up in a 37°C, 5% CO2 chamber. Cells are treated with TRAIL at 0, 20, 40, and 80 ng/mL or chlorambucil at 0, 2.5, 5, and 10 μM for 48 hours after attached growth for 24 hours. After adding 10 μL of CCK-8 reagent to each well, the mixture is incubated for 4 hours at 37°C. Subsequently, a micro-plate reader measures the absorbance values at 450 nm. For every treatment group, six parallel samples are run. Rate of cell proliferation (%) = mean value of control group × 100% / mean value of experimental group[1].
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| Animal Protocol |
Mice: Swiss female mice are split into five groups at random (20 mice in each group). Group 1 is maintained as the control group. Group 2 is administered 2.5 × 106 Ehrlich ascites carcinoma cells intraperitoneally. Group 3 is given oral treatment with chlorambucil at a dose of 0.2 mg/kg body weight. Group 4 is given oral treatment with levamisole at a dose of 5 mg/kg body weight. Group 5 is given daily oral treatment with a combination of chlorambucil and levamisole, administered through a bent stainless steel stomach tube[2].
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| References |
[1]. Guo JX, et al. Synergistic effects of chlorambucil and TRAIL on apoptosis and proliferation of Raji cells. Eur Rev Med Pharmacol Sci. 2017 Oct;21(20):4703-4710.
[2]. Salem FS, et al. Biochemical and pathological studies on the effects of levamisole and chlorambucil on Ehrlich ascites carcinoma-bearing mice. Vet Ital. 2011 Jan-Mar;47(1):89-95. [3]. Mohamed D, et al. Chlorambucil-adducts in DNA analyzed at the oligonucleotide level using HPLC-ESI MS. Chem Res Toxicol. 2009;22(8):1435-1446. [4]. Birnbaum AD, et al. Chlorambucil and malignancy. Ophthalmology. 2010;117(7):1466-1466.e1 |
| Molecular Formula |
C14H19CL2NO2
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| Molecular Weight |
304.21
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| Exact Mass |
303.08
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| Elemental Analysis |
C, 55.27; H, 6.30; Cl, 23.31; N, 4.60; O, 10.52
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| CAS # |
305-03-3
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| Related CAS # |
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| Appearance |
Pale brown to brown solid powder
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| SMILES |
C1=CC(=CC=C1CCCC(=O)O)N(CCCl)CCCl
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| InChi Key |
JCKYGMPEJWAADB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H19Cl2NO2/c15-8-10-17(11-9-16)13-6-4-12(5-7-13)2-1-3-14(18)19/h4-7H,1-3,8-11H2,(H,18,19)
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| Chemical Name |
4-[4-[bis(2-chloroethyl)amino]phenyl]butanoic acid
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| Synonyms |
CB-1348; WR-139013; CB1348; WR139013; CB 1348; WR 139013; chlorambucilum; chloraminophen; Chlorbutin; chlorbutine; chlorbutinum; chloroambucil; chlorobutin; chlorobutine; Leukersan; Leukoran; Lympholysin; phenylbutyric acid nitrogen mustard; US brand names: Ambochlorin; Amboclorin; Leukeran; Linfolizin. Foreign brand names: Altichlorambucil; Chloraminophene; Linfolysin.
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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 |
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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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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2872 mL | 16.4360 mL | 32.8720 mL | |
| 5 mM | 0.6574 mL | 3.2872 mL | 6.5744 mL | |
| 10 mM | 0.3287 mL | 1.6436 mL | 3.2872 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 |
| NCT02242942 | Active Recruiting |
Drug: Chlorambucil Drug: Venetoclax |
Lymphocytic Leukemia, Chronic | Hoffmann-La Roche | December 31, 2014 | Phase 3 |
| NCT03462719 | Active Recruiting |
Drug: Ibrutinib Drug: Venetoclax |
Leukemia, Lymphocytic, Chronic, B-Cell |
Janssen Research & Development, LLC |
April 17, 2018 | Phase 3 |
| NCT04075292 | Active Recruiting |
Drug: Acalabrutinib Drug: Rituximab |
Untreated Chronic Lymphocytic Leukemia |
AstraZeneca | January 20, 2020 | Phase 3 |
| NCT02475681 | Active Recruiting |
Drug: Acalabrutinib Drug: Obinutuzumab |
Chronic Lymphocytic Leukemia | Acerta Pharma BV | June 26, 2015 | Phase 3 |
| NCT04692740 | Active Recruiting |
Drug: Chlorambucil, Oral, 2 Mg | Pancreatic Ductal Adenocarcinoma | Michele Reni | December 18, 2020 | Phase 2 |
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