Clofarabine

SKU: orb1226718

Description

Clofarabine(Clolar; Clofarex) inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase.(In Vitro):Clofarabine potently inhibits DNA synthesis. Clofarabine demonstrates strong in vitro growth inhibition and cytotoxic activity (IC50 values=0.028-0.29 μM) in a wide variety of leukaemia and solid tumour cell lines.Clofarabine (0.01-0.1 μM) inhibits proliferation of NB4 cells, which may be related with the down-regulation of Bcl-2 and induction of apoptosis.(In Vivo):Clofarabine (330 mg/kg, after a 7-day treatment) causes the death of mice. Higher mortality rates were observed in daytime treatment groups, while more animals survived in night treatment groups. Significant differences of LD50 are found at various time points especially at 12:00 noon and 12:00 midnight.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 123318-82-1
• MW: 303.68
• Purity: >98% (HPLC)
• Formula: C₁₀H₁₁ClFN₅O₃
• SMILES: O[C@H]1[C@H](CO)O[C@@H](N2C=NC3=C(N)N=C(Cl)N=C23)[C@@H]1F
• Target: DNA/RNA Synthesis
• Solubility: DMSO: 60 mg/mL (197.57 mM)

Bioactivity

• In Vivo:
  Clofarabine (330 mg/kg, after a 7-day treatment) causes the death of mice. Higher mortality rates were observed in daytime treatment groups, while more animals survived in night treatment groups. Significant differences of LD50 are found at various time points especially at 12: 00 noon and 12: 00 midnight. Animal model: Kunming mice (18-22 g, with equal numbers of male and female mice). Dosage: 600, 480, 384, 307, 246 mg/kg. Administration: Injected intraperitoneally at 8: 00 am, 12: 00 noon, 8: 00 pm and 12: 00 midnight; 7 days continuous administration. Result: LD50s of 8: 00 am, 12: 00 noon, 8: 00 pm, 12: 00 midnight were 333.59, 319.73, 362.58 and 366.92 mg/kg, respectively.
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• In Vitro:
  Clofarabine potently inhibits DNA synthesis. Clofarabine demonstrates strong in vitro growth inhibition and cytotoxic activity (IC50 values=0.028-0.29 μM) in a wide variety of leukaemia and solid tumour cell lines. Clofarabine (0.01-0.1 μM) inhibits proliferation of NB4 cells, which may be related with the down-regulation of Bcl-2 and induction of apoptosis. Cell Viability Assay Cell line: NB4 cells. Concentration: 0.01-0.1 μM Incubation time: 48 hours. Result: Inhibited proliferation of NB4 cells in a concentration-depended manner. Apoptosis Analysis Cell line: NB4 cells. Concentration: 0.01-0.1 μM Incubation time: 24 hours. Result: Apoptosis rate increased obviously. Western blot analysis. Cell line: NB4 cells. Concentration: 0.01-0.1 μM Incubation time: 24 hours. Result: Bcl-2 expression decreased obviously.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Clolar | Evoltra

Quick Database Links

Gene Symbol

DNA/RNA Synthesis