Cyclophosphamide inhibits the AChE reversibly with an IC50 of 511 microM. The Michaelis-Menten constant (Km) was 132 microM for AChE in the control system; a value increased by 78% in the CP treated system. The Vmax was 73.8 mumol/h/mg protein for the control system. Cyclophosphamide is used to treat cancers and autoimmune disorders. Cyclophosphamide belongs to a group of drugs called alkylating agents. It works by sticking to one of the cancer cell's DNA strands. DNA is the genetic code that is in the heart of all animal and plant cells. It controls everything the cell does.The cell cannot then divide into 2 new cells.
*The compound is unstable in solutions, freshly prepared is recommended
 |
Source | Mol Cancer Ther (2015). Figure 5.Cyclophosphamide |
| Method | i.p. | |
| Cell Lines | NCR/nu and nu/nu nude mice | |
| Concentrations | 170 mg/kg | |
| Incubation Time | 24 h | |
| Results | Cyclophosphamide induced a significant increase of DiI5-liposome MFI at each of the distances from blood vessels analyzed. |
 |
Source | Mol Cancer Ther (2015). Figure 1.Cyclophosphamide |
| Method | i.p. | |
| Cell Lines | NCR/nu and nu/nu nude mice | |
| Concentrations | 170 mg/kg | |
| Incubation Time | 24 h | |
| Results | BT474-M3 tumor–bearing mice were predosed with cyclophosphamide (170 mg/kg) 2 to 5 days before injection of HER2-tPLD or free doxorubicin (both at 3 mg/kg). |
| Cell Experiment | |
|---|---|
| Cell lines | CD4+ T-cell |
| Preparation method | Total CD4+ T cells, labeled with αCD25 BV605, were cultured for 3 days in RPMI/10% AB containing 0 or 50 IU/mL IL-2 as indicated, in presence of CPA (0 μM-1000 μM), mafosfamide (MAF; stabilized active derivative of CPA) (0 μM, 1.2 μM, 12 μM), and/or verapamil (10 μM). Doses of CPA and MAF were titrated to identify doses discriminating sensitivity of Treg and non-Treg cell subsets. |
| Concentrations | 0 μM, 1.2 μM, 12 μM |
| Incubation time | 3 d |
| Animal Experiment | |
|---|---|
| Animal models | Sprague–Dawley rats |
| Formulation | |
| Dosages | 25mg/kg |
| Administration | i.v. |
| Molecular Weight | 261.09 |
| Formula | C7H15Cl2N2O2P |
| CAS Number | 50-18-0 |
| Solubility (25°C) | DMSO 35 mg/mL Water 30 mg/mL |
| Storage | 2-8°C |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] al-Jafari AA, et al. Toxicology. Inhibition of human acetylcholinesterase by cyclophosphamide.
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