Clofarabine inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase. Induces apoptosis by directly altering mitochondrial transmembrane potential. Demonstrates growth inhibition and cytotoxic activity in a variety of leukemias and solid tumors.
| Cell Experiment | |
|---|---|
| Cell lines | hela cells |
| Preparation method | Radiosensitivity assay. Cells were treated with indicated dose of clofarabine, and then media was changed 20 hours later. The cultures were incubated for 10-12 days, harvested, and stained with 0.5% crystal violet in methanol. The colony number was determined with a dissecting microscope. a population of >50 cells was counted as one colony, and the number of colonies was expressed as a percentage of the value for untreated controls and those treated with clofarabine. the survival curves were plotted by linear regression analyses, and the D0 value represents the radiation dose that lead to 37% survival. |
| Concentrations | 0, 10, 100, and 1000 n M |
| Incubation time | 4h |
| Animal Experiment | |
|---|---|
| Animal models | male nude mice bearing DLD-1 human tumour xenografts model |
| Formulation | DMSO/H2O |
| Dosages | 30mg/kg daily for 12 days |
| Administration | i.p. |
| Molecular Weight | 303.68 |
| Formula | C10H11ClFN5O3 |
| CAS Number | 123318-82-1 |
| Solubility (25°C) | DMSO 33 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
[1] Ghanem et al. Leuk Lymphoma. The Role of Clofarabine in Acute Myeloid Leukemia.
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