货号:A568740 同义名: 阿糖胞苷 / Cytosine β-D-arabinofuranoside;Cytosine Arabinoside
Cytarabine是一种核苷类似物,诱导S期细胞周期停滞并抑制DNA聚合酶。它以16 nM的IC50抑制DNA合成,并对HSV具有抗病毒作用。阿糖胞苷还表现出抗正痘病毒的活性。
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产品名称 | DNA synthesis ↓ ↑ | helicase ↓ ↑ | RdRp ↓ ↑ | ribonucleotide reductase ↓ ↑ | tRNA synthetase ↓ ↑ | YB-1 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Fexinidazole | ✔ | 98% | |||||||||||||||||
Daptomycin | ✔ | 98% | |||||||||||||||||
Blasticidin S·HCl | ✔ | 98% | |||||||||||||||||
Metronidazole | ✔ | 98% | |||||||||||||||||
Daunorubicin HCl |
+++
DNA synthesis, Ki: 20 nM |
98% | |||||||||||||||||
Triglycidyl isocyanurate | ✔ | p53 | 98+% | ||||||||||||||||
Nedaplatin | ✔ | 99%+ | |||||||||||||||||
Bendamustine | ✔ | 98+% | |||||||||||||||||
Trifluridine | ✔ | 98% | |||||||||||||||||
Robinetin | ✔ | 99%+ | |||||||||||||||||
Carboplatin | ✔ | 99% | |||||||||||||||||
Cidofovir | ✔ | 99% | |||||||||||||||||
Cisplatin | ✔ | 99% | |||||||||||||||||
Cytarabine |
++++
DNA synthesis, IC50: 16 nM |
98% | |||||||||||||||||
Acelarin |
++++
DNA synthesis, EC50: 0.2 nM |
99%+ | |||||||||||||||||
Oxaliplatin | ✔ | 98% | |||||||||||||||||
YK-4-279 | ✔ | 99%+ | |||||||||||||||||
ML216 |
+
BLM636-1298, IC50: 0.97 μM BLMfull-length, IC50: 2.98 μM |
99%+ | |||||||||||||||||
RK-33 | ✔ | 98% | |||||||||||||||||
Brr2-IN-3 | ✔ | 99%+ | |||||||||||||||||
Phen-DC3 Trifluoromethanesulfonate | ✔ | 98% | |||||||||||||||||
Favipiravir | ✔ | 97% | |||||||||||||||||
Suramin sodium salt |
++
RdRp, IC50: 0.26 μM |
99%+ | |||||||||||||||||
Clofarabine |
++
Ribonucleotide reductase, IC50: 65 nM |
97% | |||||||||||||||||
Didox | ✔ | 98% | |||||||||||||||||
(E)-3-AP | ✔ | 97% | |||||||||||||||||
Halofuginone |
+++
prolyl-tRNA synthetase, Ki: 18.3nM |
99%+ | |||||||||||||||||
BC-LI-0186 |
+++
Leucyl-tRNA synthetase, Kd: 42.1 nM Leucyl-tRNA synthetase, IC50: 46.11 nM |
98% | |||||||||||||||||
SU056 |
+
YB-1, IC50: 1.73 μM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Cytarabine (Ara-C) is an antineoplastic and antileukemic agent in current clinical treatment. Cytarabine belongs to a class of nucleoside-analogue antimetabolite, which can enter into cells and be phosphorylated by deoxynucleoside salvage pathway and produce their activity by being incorporated into DNA during replication or repair, leading to inhibition of chain extension[1]. Cytarabine, combined with other drugs, is mainly used in the treatment for acute lymphoblastic leukemia (ALL), acute myeloid leukemia (AML) and chronic myelogenous leukemia (CML) (see https://www.fda.gov/), also can be used in treatment for other cancer. Cytarabine can inhibit DNA synthesis mainly through being incorporated into cellular DNA by both repair and replication synthesis[2]. Cytarabine can induce apoptosis, s phase arrest, as well as cell growth inhibition[3]. Cytarabine is usually used in long-term neuron culture to reduce glial cells and enhance neurons for its mitotic inhibition[4]. |
作用机制 | Cytarabine, as nucleoside analogue, can inhibit DNA synthesis mainly through being incorporated into cellular DNA by both repair and replication synthesis. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
CCRF-CEM cell line | Function assay | Inhibit the replication of CCRF-CEM cell line in vitro, ED50=5 nM. | 1995894 | ||
CCRF-CEM cell lines | Function assay | 72 h | Concentration required to inhibit replication of CCRF-CEM cell lines by 50% after 72 hr incubation, ED50=6 nM. | 1652024 | |
CCRF-CEM human leukemic lymphoblastoid cell lines | Cytotoxic assay | Cytotoxicity against CCRF-CEM human leukemic lymphoblastoid cell lines, IC50=20 nM. | 6827546 | ||
HeLa human cell lines | Function assay | 144 h | The compound was tested in vitro for antitumor activity(50% inhibition of tumor cell growth) against HeLa human cell lines after 144 hr, ID50=0.1 μM | 3625714 | |
Dose | Mice: 50 mg/kg, 100 mg/kg[5] (i.p.); 20 mg/kg, 60 mg/kg[6] (s.c.) |
Administration | i.p., s.c. |
Pharmacokinetics |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.11mL 0.82mL 0.41mL |
20.56mL 4.11mL 2.06mL |
41.12mL 8.22mL 4.11mL |
CAS号 | 147-94-4 |
分子式 | C9H13N3O5 |
分子量 | 243.21 |
别名 | 阿糖胞苷 ;Cytosine β-D-arabinofuranoside;Cytosine Arabinoside;U-19920A;NSC 287459;NSC 63878;1-β-D-Arabinofuranosylcytosine;Ara-C |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,Room Temperature |
溶解度 |
DMSO: 16 mg/mL(65.78 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 45 mg/mL(185.02 mM),配合低频超声助溶 |
动物实验配方 |