2. Cell Cycle/DNA Damage
  3. DNA Alkylator/Crosslinker
  4. Chlorambucil

Chlorambucil  (Synonyms: CB-1348; WR-139013)

Cat. No.: HY-13593 Purity: 99.64%
SDS COA Handling Instructions

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Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease.

For research use only. We do not sell to patients.

Chlorambucil Chemical Structure

Chlorambucil Chemical Structure

CAS No. : 305-03-3

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10 mM * 1 mL in DMSO
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Based on 4 publication(s) in Google Scholar

Other Forms of Chlorambucil:

Chlorambucil Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease[1][2][3][4].

IC50 & Target

DNA Alkylator[1]
In Vitro

Chlorambucil can deprive the function of complementary strands of DNA molecules via alkalization-induced cross interaction, and then inhibits tumor cell proliferation. Chlorambucil (0, 2.5, 5, 10 μM) exhibits slight inhibitory effect on Raji cell apoptosis, but potently increases DR4 and DR5 mRNA expression in Raji cells. Chlorambucil (10 μM) in combination with Tumor necrosis factor (TNF) related apoptosis inducing ligand (TRAIL, 80 ng/ml) has synergistic effect on Raji cell apoptosis and inhibition on proliferation[1].
Chlorambucil is a DNA alkylator at high doses and, at lower doses, acts as an inhibitor of synthesis of nuclear proteins, particularly histones. Increasing doses are associated with a higher frequency of apoptosis, whereas long-term maintenance therapy has been associated with mutations of the p53 gene, leading to secondary malignancies[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chlorambucil Related Antibodies
In Vivo

Chlorambucil (0.2 mg/kg, p.o.) in combination with levamisole (5 mg/kg) has enhanced anti-cancer effect on Ehrlich ascites carcinoma which elevates apoptosis of Ehrlich ascites carcinoma and the survival rate of the mice. However, Chlorambucil exhibits adverse effects on the liver and kidneys of mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

304.21

Formula

C14H19Cl2NO2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(O)CCCC1=CC=C(N(CCCl)CCCl)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 24 mg/mL (78.89 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.84%

SDS (584 KB)

COA (247 KB) LCMS (119 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

Cultured cells at log-growth phase are digested by trypsin into single cell suspension and are seeded into 96-well plate at 1000 per well density. The plate is placed in a 37°C chamber with 5% CO2. After attached growth for 24 h, 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 h. 10 μL CCK-8 reagent is added to each well, followed by incubation at 37°C for 4 h. Absorbance values at 450 nm are then measured by a micro-plate reader. Six parallel samples are performed in each treatment group. Cell proliferation rate (%) = mean value of experimental group/mean value of control group × 100%[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
Female Swiss mice are divided randomly into five group (20 mice per group). Group 1 is kept as the control group, Group 2 receives intraperitoneal injection of by 2.5 × 106 Ehrlich ascites carcinoma cell, Gropu 3 is treated orally with Chlorambucil 0.2 mg/kg body weight, Group 4 is treated orally with levamisole (5 mg/kg body weight) and Group 5 is treated orally with a combination of Chlorambucil and levamisole each day, using a bent stainless steel stomach tube[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2872 mL 16.4360 mL 32.8720 mL 82.1801 mL
5 mM 0.6574 mL 3.2872 mL 6.5744 mL 16.4360 mL
10 mM 0.3287 mL 1.6436 mL 3.2872 mL 8.2180 mL
15 mM 0.2191 mL 1.0957 mL 2.1915 mL 5.4787 mL
20 mM 0.1644 mL 0.8218 mL 1.6436 mL 4.1090 mL
25 mM 0.1315 mL 0.6574 mL 1.3149 mL 3.2872 mL
30 mM 0.1096 mL 0.5479 mL 1.0957 mL 2.7393 mL
40 mM 0.0822 mL 0.4109 mL 0.8218 mL 2.0545 mL
50 mM 0.0657 mL 0.3287 mL 0.6574 mL 1.6436 mL
60 mM 0.0548 mL 0.2739 mL 0.5479 mL 1.3697 mL
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Chlorambucil Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Chlorambucil305-03-3CB-1348 WR-139013CB1348CB 1348WR139013WR 139013WR-139013DNA Alkylator/CrosslinkerDNAalkylatornuclearproteinshistonesmutationsp53malignanciesInhibitorinhibitorinhibit

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