Clofarabine

Research use only, not for human use.

Clofarabine(Clolar; Clofarex) inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase.

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.

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 hoursResult:Bcl-2 expression decreased obviously.

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.

Clolar | Evoltra

Cell Cycle/DNA Damage

DNA/RNA Synthesis

RR

Cancer

——

123318-82-1

303.68

C10H11ClFN5O3

>98% (HPLC)

DMSO: 60 mg/mL (197.57 mM)

O[C@H]1[C@H](CO)O[C@@H](N2C=NC3=C(N)N=C(Cl)N=C23)[C@@H]1F

(2S,3S,4R,5R)-5-(6-amino-2-chloro-9H-purin-9-yl)-4-fluoro-2-(hydroxymethyl)tetrahydrofuran-3-ol

(-20℃)

With Ice Pack

≥ 2 years