1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECytarabine hydrochlorideCat. No.: HY-13605ACAS No.: 69-74-9Synonyms: Cytosine -D-arabinofuranoside hydrochloride; CytosineArabinoside hydrochloride; Ara-C hydrochloride分式: CHClNO分量: 279.68作靶點(diǎn): DNA/RNA Synthesis; Nucleoside Antim

2、etabolite/Analog;Autophagy作通路: Cell Cycle/DNA Damage; Autophagy儲(chǔ)存式: Please store the product under the recommended conditions inthe COA.BIOLOGICAL ACTIVITY物活性 Cytarabine (AraC) 鹽酸鹽種核苷類似物，可引起 S 期細(xì)胞周 期停滯并抑制 DNA聚合酶。Cytarabine 抑制DNA 合成的 IC50 為 16 nM。IC50 & Target IC50: 16 nM (DNA synthesis)體外研究 Cytarabi

3、ne 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 wild-t

4、ype 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 mitochondrial

5、cytochrome-cand the activation of caspase-3, and the toxicity can be attenuated by p53 knockdown and delayed by baxdeletion 2.體內(nèi)研究Cytarabine (250 mg/kg) also causes placental growth retardation and increases placental trophoblastic cellsapoptosis in the placental labyrinth zone of the pregnant Slc:W

6、istar 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 leuka

7、emias, which causes the chCytarabineteristic G1/Sblockage and synchronization, and increases the survival time for leukaemic Brown Norway rats in a weak1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEdose-related fashion indicating that the use of higher dosages of Cytarabine does not contribute to

8、 itsantileukaemic effectiveness in man 4.PROTOCOLKinase 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 s

9、uspended in their respective media to give 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 -f

10、ree medium, and final cell counts are determined. 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 con

11、firmed the accuracy of these methods. They are 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

12、 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.

13、with an equivalent volume ofPBS on GD13 and killed 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 c

14、onfirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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 / www.Me

15、dChemEREFERENCES1. 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 insympatheti

16、c 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. 1762-7.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE4. 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 retrospective c