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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 |
[1] Ghanem et al. Leuk Lymphoma. The Role of Clofarabine in Acute Myeloid Leukemia.
| Related DNA/RNA Synthesis Products |
|---|
| Gemcitabine Hydrochloride
Gemcitabine (Gemzar, LY188011) inhibits DNA synthesis with an IC50 of 0.06 µM. |
| Nelarabine
Nelarabine is a novel purine antimetabolite antineoplastic agent. |
| Mizoribine
Mizoribine (Bredinin) is an imidazole nucleoside and an immunosuppressive agent with an IC50 of approximately 100 μM. Mizoribine inhibits replication of SARS-CoV with IC50s of 3.5 μg/mL and 16 μg/mL for SARS-CoV Frankfurt-1 and SARS-CoV HKU39849, respectively. |
| Capecitabine
Capecitabine is an orally-administered chemotherapeutic agent. Capecitabine is a precursor, that is enzymatically converted to 5-fluorouracil in the tumor, where it inhibits DNA synthesis and slows growth of tumor tissue. Capecitabine may inhibit cytochrome CYP2C9 enzyme, and therefore increase levels of substrates such as phenytoin and other substrates of CYP2C9. |
| Temozolomide
Temozolomide (TMZ) is an oral DNA methylating, chemotherapeutic agent. |
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