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Cytarabine
| Product Name | Cytarabine |
| Price: | $18 / 20mg |
| Catalog No.: | CN00268 |
| CAS No.: | 147-94-4 |
| Molecular Formula: | C9H13N3O5 |
| Molecular Weight: | 243.22 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | OC[C@H]1O[C@H]([C@H]([C@@H]1O)O)n1ccc(nc1=O)N |
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| Description | Cytarabine is a chemotherapy drug used to treat acute myeloid leukaemia, acting by inhibiting DNA synthesis with an IC50 of 16 nM. |
| Target | IC50: 16 nM (DNA synthesis) |
| In Vitro | Cytarabine is phosphorylated into a triphosphate form (Ara-CTP) involving deoxycytidine kinase (dCK), which competes with dCTP for incorporation into DNA, and then blocks DNA synthesis by inhibiting the function of DNA and RNA polymerases. Cytarabine displays a higher growth inhibitory activity towards wild-type CCRF-CEM cells compared to other acute myelogenous leukemia (AML) cells with IC50 of 16 nM[1]. Cytarabine apparently induces apoptosis of rat sympathetic neurons at 10 μM, of which 100 μM shows the highest toxicity and kills over 80% of the neurons by 84 hours, involving the release of mitochondrial cytochrome-c and the activation of caspase-3, and the toxicity can be attenuated by p53 knockdown and delayed by bax deletion[2]. |
| In Vivo | Cytarabine (250 mg/kg) also causes placental growth retardation and increases placental trophoblastic cells apoptosis in the placental labyrinth zone of the pregnant Slc:Wistar rats, which increases from 3 hour after the treatment and peaks at 6 hour before returning to control levels at 48 hour, with remarkably enhanced p53 protein, p53 trancriptional target genes such as p21, cyclinG1 and fas and caspase-3 activity[3]. Cytarabine is highly effective against acute leukaemias, which causes the Cytarabine teristic G1/S blockage and synchronization, and increases the survival time for leukaemic Brown Norway rats in a weak dose-related fashion indicating that the use of higher dosages of Cytarabine does not contribute to its antileukaemic effectiveness in man[4]. |
| Animal Admin | Pregnant rats are injected intraperitoneally (i.p.) with 250 mg/kg of Cytarabine on Day 13 of gestation (GD13). Under the conditions of this experiment, congenital anomalies and growth retardation are detected at a high rate in perinatal fetuses, although the incidence of fetal death is not markedly increased. At 1, 3, 6, 9, 12, 24, and 48 h after the treatment, six dams each are killed by heart puncture under ether anesthesia, and the placentas are collected. As controls, six pregnant rats are injected i.p. with an equivalent volume of PBS on GD13 and killed at the same time point as Cytarabine-treated groups. Of the six dams obtained at each time point, three are used for histopathological analyses and three for reverse transcription-polymerase chain reaction (RT-PCR) analysis. |
| Density | 1.9±0.1 g/cm3 |
| Boiling Point | 529.7±60.0 °C at 760 mmHg |
| Flash Point | 274.1±32.9 °C |
| Exact Mass | 243.085526 |
| PSA | 130.83000 |
| LogP | -1.78 |
| Vapour Pressure | 0.0±3.2 mmHg at 25°C |
| Storage condition | 2-8°C |