Cyclophosphamide monohydrate |
| Catalog No.GC14077 |
An alkylating agent
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 6055-19-2
Sample solution is provided at 25 µL, 10mM.
IC50: 511 μM for AChE
Cyclophosphamide monohydrate is used in the cancer treatment in children. As a prodrug it should be metabolized by cytochrome P-450 enzymes to produce the active alkylating species, which are responsible for its cytotoxic effects.
In vitro: Cyclophosphamide inhibited the AChE reversibly with an IC50 of 511 μM. In the control system, Km was 132 μM for AChE, which increased by 78% in the CP treated system. The nature of cyclophosphamide was of the linear mixed type (partially competitive and purely noncompetitive). The values of Ki and KI were estimated to be 378 and 582 μM respectively, indicating that noncompetitive inhibition was predominant over competitive [1].
In vivo: PK studies in mice revealed a delayed plasma clearance of cyclophosphamide after carbon-tetrachloride pretreatment. Plasma levels of total alkylating activity and 4-hydroxycyclophosphamide increased more slowly and reached a lower peak. However, there was no difference in the AUC for either plasma total alkylating activity or plasma 4-hydroxycyclophosphamide between two groups. Thus, prolonged exposure of tumor cells to 4-hydroxycyclophosphamide might be responsible for the increased antitumor activity of cyclophosphamide following carbon-tetrachloride pretreatment [2].
Clinical trial: Twenty-two children not receiving other therapy known to influence drug metabolism were selected, of whom, nine were receiving combination treatment and thirteen were identified as controls. Results showed that the the plasma cyclophosphamide clearance was lower in patients receiving fluconazole combined group [3].
References:
[1] al-Jafari AA,Duhaiman AS,Kamal MA. Inhibition of human acetylcholinesterase by cyclophosphamide. Toxicology.1995 Jan 19;96(1):1-6.
[2] Harris RN,Basseches PJ,Appel PL,Durski AM,Powis G. Carbon tetrachloride-induced increase in the antitumor activity of cyclophosphamide in mice: a pharmacokinetic study. Cancer Chemother Pharmacol.1984;12(3):167-72.
[3] Yule SM,Walker D,Cole M,McSorley L,Cholerton S,Daly AK,Pearson AD,Boddy AV. The effect of fluconazole on cyclophosphamide metabolism in children. Drug Metab Dispos.1999 Mar;27(3):417-21.
| Cas No. | 6055-19-2 | SDF | |
| Chemical Name | N,N-bis(2-chloroethyl)-2-oxo-1,3,2λ5-oxazaphosphinan-2-amine;hydrate | ||
| Canonical SMILES | C1CNP(=O)(OC1)N(CCCl)CCCl.O | ||
| Formula | C7H15Cl2N2O2P.H2O | M.Wt | 279.1 |
| Solubility | ≥ 13.95 mg/mL in DMSO, ≥ 96 mg/mL in EtOH, ≥ 51.5 mg/mL in Water with ultrasonic and warming. This product is unstable in solution and it is recommended to prepare and use it immediately. | Storage | Store at -20°C,unstable in solution, ready to use. |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.5829 mL | 17.9147 mL | 35.8295 mL |
| 5 mM | 0.7166 mL | 3.5829 mL | 7.1659 mL |
| 10 mM | 0.3583 mL | 1.7915 mL | 3.5829 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *