Cytarabine-Cytosine-β-D-arabinofuranoside-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECytarabineCat. No.: HY-13605CAS No.: 147-94-4Synonyms: Cytosine -D-arabinofuranoside; Cytosine Arabinoside; Ara-C分式: CHNO分量: 243.22作靶点: DNA/RNA Synthesis; Nucleoside Antimetabolite/Analog;Autophagy作通路: Cell Cycle/DNA Damage; Aut

2、ophagy储存式: -20C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性数据体外实验 H2O : 48 mg/mL (197.35 mM; Need ultrasonic)DMSO : 17.3 mg/mL (71.13 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 4.1115 mL 20.5575 mL 41.1150 mL5 mM 0.82

3、23 mL 4.1115 mL 8.2230 mL10 mM 0.4112 mL 2.0558 mL 4.1115 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Cytarabine种核苷类似物，可引起 S 期细胞周 期停滞并抑制 DNA聚合酶。Cytarabine 抑制DNA 合成的IC50为16 nM。IC50 & Target IC50: 16 nM (DNA synthesis)1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 Cytar

4、abine is phosphorylated into a triphosphate form (Ara-CTP) involving deoxycytidine kinase (dCK), whichcompetes with dCTP for incorporation into DNA, and then blocks DNA synthesis by inhibiting the function ofDNA and RNA polymerases. Cytarabine displays a higher growth inhibitory activity towards wil

5、d-type CCRF-CEM cells compared to other acute myelogenous leukemia (AML) cells with IC50 of 16 nM 1. Cytarabineapparently induces apoptosis of rat sympathetic neurons at 10 M, of which 100 M shows the highesttoxicity and kills over 80% of the neurons by 84 hours, involving the release of mitochondri

6、al cytochrome-cand the activation of caspase-3, and the toxicity can be attenuated by p53 knockdown and delayed by baxdeletion 2.体内研究 Cytarabine (250 mg/kg) also causes placental growth retardation and increases placental trophoblastic cellsapoptosis in the placental labyrinth zone of the pregnant S

7、lc:Wistar rats, which increases from 3 hour afterthe treatment and peaks at 6 hour before returning to control levels at 48 hour, with remarkably enhancedp53 protein, p53 trancriptional target genes such as p21, cyclinG1 and fas and caspase-3 activity 3.Cytarabine is highly effective against acute l

8、eukaemias, which causes the Cytarabine teristic G1/S blockageand 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 itsantileukaemic effectiveness in man 4.PROT

9、OCOLKinase Assay 1 Stock solution of Cytarabine is prepared in absolute ethanol, and serial dilutions of Cytarabine are prepared.CCRF-CEM cells are suspended in RPMI medium supplemented with 10% FBS, 0.1% gentamicin, and 1%sodium pyruvate. The cells are suspended in their respective media to give 10

10、 mL volumes of cellsuspension at a final density of 3-6104 cells/mL. Appropriate volumes of Cytarabine solution are transferredto the cell suspensions, and incubation is continued for 72 hours. The cells are spun down and resuspendedin fresh Cytarabine -free medium, and final cell counts are determi

11、ned. The data are analyzed by sigmoidalcurve fitting of the cell count versus Cytarabine concentration, and the results are expressed as the IC50(Cytarabine concentration that inhibits cell growth to 50% of the control value).MCE has not independently confirmed the accuracy of these methods. They ar

12、e for reference only.Animal Pregnant rats are injected intraperitoneally (i.p.) with 250 mg/kg of Cytarabine on Day 13 of gestationAdministration 3 (GD13). Under the conditions of this experiment, congenital anomalies and growth retardation are detectedat a high rate in perinatal fetuses, although t

13、he 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 ofPBS on GD13 and k

14、illed at the same time point as Cytarabine-treated groups. Of the six dams obtained ateach time point, three are used for histopathological analyses and three for reverse transcription-polymerasechain reaction (RT-PCR) analysis.MCE has not independently confirmed the accuracy of these methods. They

15、are for reference only.户使本产品发表的科研献2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE Cell. 2018 Sep 20;175(1):171-185.e25. J Mol Med (Berl). 2019 Jun 14. Fish Shellfish Immunol. 2019 Jul 9. pii: S1050-4648(19)30726-0. SLAS Discov. 2018 Aug;23(7):687-696.See more customer validations on HYPERLINK / ww

16、w.MedChemEREFERENCES1. Tobias, S.C. and R.F. Borch, Synthesis and biological evaluation of a cytarabine phosphoramidate prodrug. Mol Pharm, 2004. 1(2): p.112-6.2. Besirli, C.G., et al. Cytosine arabinoside rapidly activates Bax-dependent apoptosis and a delayed Bax-independent death pathway insympat

17、hetic neurons. Cell Death Differ, 2003. 10(9): p. 1045-58.3. Yamauchi, H., et al., Involvement of p53 in 1-beta-D-arabinofuranosylcytosine-induced trophoblastic cell apoptosis and impairedproliferation in rat placenta. Biol Reprod, 2004. 70(6): p. 1762-7.4. Richel, D.J., et al., Comparison of the antileukaemic activity of 5 aza-2-deoxycytidine and arabinofuranosyl-cytosine in rats withmyelocytic leukaemia. Br J Cancer, 1988. 58(6): p. 730-3.5. Shepshelovich D, et al. Pharmacodynamics of cytarabine induced leucopenia: a re