Carmustine (BiCNU) is a cell-cycle phase nonspecific alkylating antineoplastic agent with ED50 ranging from 5.0 µM to 11.9 µM. It is used in the treatment of several types of brain cancer (including glioma, glioblastoma multiforme, medulloblastoma and astrocytoma), multiple myeloma and lymphoma (Hodgkin’s and non-Hodgkin). In a study, three lines with O6-AGT activity below 25 fmol/mg protein had carmustine ED50 values ranging from 5.0 µM to 11.9 µM.
| Molecular Weight | 214.05 |
| Formula | C5H9Cl2N3O2 |
| CAS Number | 154-93-8 |
| Solubility (25°C) | DMSO |
| Storage | -20°C, protect from light |
| 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.
[4] Alison B Fleming, et al. Pharmacokinetics of the carmustine implant
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4-Hydroperoxy cyclophosphamide, the active metabolite form of the precursor Cyclophosphamide, cross-links DNA and induces T-cell apoptosis independent of caspase receptor activation, as well as activating the mitochondrial death pathway through the generation of reactive oxygen species (ROS). It can be used in studies related to rheumatoid arthritis and autoimmune diseases. |
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