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Clofarabine

Cat. No. M1698
Clofarabine Structure
Synonym:

Clolar, Evoltra

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 45  USD45 In stock
10mg USD 45  USD45 In stock
50mg USD 145  USD145 In stock
100mg USD 200  USD200 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 303.68
Formula C10H11ClFN5O3
CAS Number 123318-82-1
Purity >99%
Solubility DMSO 33 mg/mL
Storage at -20°C
References

[1] Ghanem et al. Leuk Lymphoma. The Role of Clofarabine in Acute Myeloid Leukemia.

[2] Abd Elmoneim et al. Pediatr Blood Cancer. Phase I dose-escalation trial of clofarabine followed by escalating doses of fractionated cyclophosphamide in children with relapsed or refractory acute leukemias.

[3] Thudium et al. Leuk Res. Synergism between clofarabine and decitabine through p53R2: A pharmacodynamic drug-drug interaction modeling.

[4] Aye et al. Chem Biol. Clofarabine Targets the Large Subunit (α) of Human Ribonucleotide Reductase in Live Cells by Assembly into Persistent Hexamers.

[5] Becker et al. Haematologica. Retrospective comparison of clofarabine versus fludarabine in combination with high dose cytarabine with or without granulocyte colony-stimulating factor as salvage therapies for acute myeloid leukemia.

[6] Kebriaei et al. Biol Blood Marrow Transplant. Clofarabine Combined with Busulfan Provides Excellent Disease Control in Adult Patients with Acute Lymphoblastic Leukemia Undergoing Allogeneic Hematopoietic Stem Cell Transplantation.

[7] Cariveau MJ, et al. Int J Radiat Oncol Biol Phys. Clofarabine acts as radiosensitizer in vitro and in vivo by interfering with DNA damage response.

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Keywords: Clofarabine, Clolar, Evoltra supplier, Checkpoint, inhibitors

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