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Cytarabine

Cytarabine

产品编号 T1272   CAS 147-94-4
别名: 阿糖胞苷, Ara-C, Cytosine Arabinoside, Cytosine β-D-arabinofuranoside, Arabinocytidine

Cytarabine (Ara-C) 是一种核苷类似物,一种 DNA 合成抑制剂 (IC50=16 nM)。Cytarabine 可以抑制 DNA 聚合酶,诱导细胞周期阻滞、细胞自噬凋亡。Cytarabine 具有抗肿瘤活性。

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Cytarabine Chemical Structure
Cytarabine, CAS 147-94-4
规格 价格/CNY 货期 数量
50 mg ¥ 298 现货
100 mg ¥ 418 现货
500 mg ¥ 772 现货
1 g ¥ 925 现货
1 mL * 10 mM (in DMSO) ¥ 460 现货
其他形式的 Cytarabine:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Cytarabine (T1272)
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纯度: 99.93%
纯度: 99.92%
纯度: 99.85%
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参考文献
产品描述 Cytarabine (Ara-C) is a nucleoside analog, an inhibitor of DNA synthesis (IC50=16 nM). Cytarabine inhibits DNA polymerase and induces cell cycle arrest, autophagy, and apoptosis. Cytarabine has antitumor activity.
靶点活性 DNA synthesis:16 nM
体外活性 方法:原代 AML 细胞用 Cytarabine (10-5000 nM) 处理 24 h,使用 MTT 方法检测细胞活力。
结果:Cytarabine 具有剂量依赖性的生长抑制作用,IC50 为1.12 μM。[1]
方法:人组织细胞淋巴瘤细胞 U937 用 Cytarabine (10-1000 nM) 处理 72 h,使用 Flow Cytometry 检测细胞周期情况。
结果:Cytarabine 剂量依赖性地降低了用 10 和 100 nM 处理的细胞中 G1 期的细胞比例,并增加了 S 期的比例。当以最高剂量 1000 nM 施用时,Cytarabine 引起亚 G1 期和 G2/M 期比例的显著增加。[2]
体内活性 方法:为研究 AML 的化疗耐药性,将 Cytarabine (10-60 mg/kg) 腹腔注射给携带人 AML 肿瘤的 NSG 小鼠,每天一次,持续五天。
结果:在所有接受 60 mg/kg Cytarabine 治疗的小鼠中,在治疗后 2 周出现细胞还原作用,治疗后 4-13 周复发。最低白血病负担和外周血复发时间方面,模型中存在剂量-反应关系。[3]
方法:为检测体内抗肿瘤活性,将 Cytarabine (6.25 mg/kg,每天一次) 和 sorafenib (60 mg/kg,每天两次) 腹腔注射给携带人 AML 肿瘤 U937 的 NOD-SCID-IL2R γnull 小鼠模型,每周一次或持续四十八天。
结果:Cytarabine 与 sorafenib 联合使用在体内产生了强大的抗 AML 活性。[4]
激酶实验 In Vitro Growth Inhibition Assay: 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 mL volumes of cell suspension at a final density of 3-6 × 104 cells/mL. Appropriate volumes of Cytarabine solution are transferred to the cell suspensions, and incubation is continued for 72 hours. The cells are spun down and resuspended in fresh Cytarabine -free medium, and final cell counts are determined. The data are analyzed by sigmoidal curve 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).
细胞实验 Cells are incubated in the presence of different concentrations of Cytarabine at 37 °C for 24, 48, and 72 hours. At the time of 20-, 44-, or 68-hour incubation in the presence of Cytarabine, 10 mL of cell proliferation reagent WST-1 solution is added. After 2- and 4-hour incubation with WST-1, cell metabolic activity is assessed with colorimetric changes quantified by measuring the absorbance in a spectrophotometer at 450 nm. And cell division times are calculated from eosin counting in parallel with viability assay(Only for Reference)
别名 阿糖胞苷, Ara-C, Cytosine Arabinoside, Cytosine β-D-arabinofuranoside, Arabinocytidine
分子量 243.22
分子式 C9H13N3O5
CAS No. 147-94-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 55 mg/mL (226.13 mM)

H2O: 24.3 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 4.1115 mL 20.5575 mL 41.115 mL 102.7876 mL
5 mM 0.8223 mL 4.1115 mL 8.223 mL 20.5575 mL
10 mM 0.4112 mL 2.0558 mL 4.1115 mL 10.2788 mL
20 mM 0.2056 mL 1.0279 mL 2.0558 mL 5.1394 mL
50 mM 0.0822 mL 0.4112 mL 0.8223 mL 2.0558 mL
100 mM 0.0411 mL 0.2056 mL 0.4112 mL 1.0279 mL

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TargetMol Library Books参考文献

1. Desai UN, et al. Enhancement of the cytotoxic effects of Cytarabine in synergism with Hesperidine and Silibinin in Acute Myeloid Leukemia: An in-vitro approach. J Cancer Res Ther. 2015 Apr-Jun;11(2):352-7. 2. Tomic B, et al. Cytarabine-induced differentiation of AML cells depends on Chk1 activation and shares the mechanism with inhibitors of DHODH and pyrimidine synthesis. Sci Rep. 2022 Jul 5;12(1):11344. 3. Robin L. Perry,et al. Ara-C Treatment of Acute Myeloid Leukemia Does Not Lead to Prolonged Enrichment of Stem Cells or a Cell Cycle Arrest. Blood. 2010; 116(21):2178. 4. Hu S, et al. Activity of the multikinase inhibitor sorafenib in combination with cytarabine in acute myeloid leukemia. J Natl Cancer Inst. 2011 Jun 8;103(11):893-905. 5. Yamauchi H, et al. Biol Reprod, 2004, 70(6), 1762-1767. 6. Shepshelovich D, et al. Pharmacodynamics of cytarabine induced leucopenia: a retrospective cohort study. Br J Clin Pharmacol. 2015 Apr;79(4):685-91. 7. Thieulent C, Hue E, Sutton G, et al. Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone or in combination[J]. Antiviral Research. 2020: 104931

TargetMol Library Books文献引用

1. He S, Li Y, Shi X, et al.DNA methylation landscape reveals LIN7A as a decitabine-responsive marker in patients with t (8; 21) acute myeloid leukemia.Clinical Epigenetics.2023, 15(1): 1-13. 2. Islam S, Rahaman M H, Yu M, et al.Anti-Leukaemic Activity of Rilpivirine Is Mediated by Aurora A Kinase Inhibition.Cancers.2023, 15(4): 1044. 3. Zhao Y, Zhao N, Cai Y, et al.An algal lectin griffithsin inhibits Hantaan virus infection in vitro and in vivo.Frontiers in Cellular and Infection Microbiology.2022, 12: 1813. 4. Thieulent C, Hue E, Sutton G, et al. Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone or in combination. Antiviral Research. 2020: 104931 5. Wang B, He B S, Ruan X L, et al. An integrated microfluidics platform with high-throughput single-cell cloning array and concentration gradient generator for efficient cancer drug effect screening. Military Medical Research. 2022, 9(1): 1-17. 6. Wang B, Pei J, Zhang H, et al.Dihydropyridine-derived calcium channel blocker as a promising anti-hantavirus entry inhibitor.Interventions for emerging infectious diseases.2023, 16648714. 7. He S, Li Y, Wang L, et al.DNA methylation landscape reveals GNAS as a decitabine-responsive marker in patients with acute myeloid leukemia.Neoplasia.2024, 49: 100965.
Camptothecin Angiotensin II human Neobavaisoflavone VAS 3947 ZINC69391 DEL-22379 Loganin Corilagin

相关化合物库

该产品包含在如下化合物库中:
EMA 上市药物库 抗癌上市药物库 抗癌活性化合物库 中药单体化合物库 抑制剂库 抗癌临床化合物库 抗癌药物库 药物功能重定位化合物库 核苷类化合物库 细胞重编程化合物库

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Keywords

Cytarabine 147-94-4 Apoptosis Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism Microbiology/Virology Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Endogenous Metabolite HSV Herpes simplex virus Orthopoxvirus Cytosine b-D-arabinofuranoside 阿糖胞苷 Cytosine beta-D-arabinofuranoside Ara-C Cytosine Arabinoside inhibit Cytosine β-D-arabinofuranoside Inhibitor Arabinocytidine inhibitor

 

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