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My CartCAS：147-94-4
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 147-94-4 |
| Name | Cytarabine |
| Molecular Formula | C9H13N3O5 |
| Molecular Weight | 243.22 |
| Solubility | Soluble in Water ≥10mg/mL |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 205-705-9 |
| MDL | MFCD00066487 |
| SMILES | O=C1N=C(N)C=CN1[C@H]2[C@H]([C@@H]([C@@H](CO)O2)O)O |
| InChIKey | UHDGCWIWMRVCDJ-CCXZUQQUSA-N |
| InChI | InChI=1S/C9H13N3O5/c10-5-1-2-12(9(16)11-5)8-7(15)6(14)4(3-13)17-8/h1-2,4,6-8,13-15H,3H2,(H2,10,11,16)/t4-,6-,7+,8-/m1/s1 |
| PubChem CID | 6253 |
| Target Point | DNA/RNA Synthesis |
| Passage | Cell Cycle;DNA Damage/DNA Repair |
| Background | Cytarabine can interfere with cell proliferation by inhibiting cellular DNA synthesis. Cytarabine is the most sensitive to the effects of cells in the S phase proliferation phase, and has a weaker effect on inhibiting RNA and protein synthesis. |
| Biological Activity | Cytarabine是一种用于治疗急性髓性白血病的化疗药物，抑制DNA 合成的IC50为16 nM。[1-4] |
| In Vitro | Cytarabine被磷酸化为三磷酸盐形式(Ara-CTP)，涉及脱氧胞苷激酶(dCK)，其与dCTP竞争结合到DNA中，然后通过抑制DNA和RNA聚合酶的功能阻断DNA合成。与其他急性髓性白血病(AML)细胞相比，Cytarabine对野生型CCRF-CEM细胞显示出更高的生长抑制活性，IC50为16 nM [1]。Cytarabine明显诱导大鼠交感神经元凋亡10μM，其中100μM显示最高毒性，并在84小时内杀死超过80％的神经元，包括线粒体细胞色素c的释放和caspase-3的激活，以及通过p53敲低可以减弱毒性，并通过bax缺失延迟[2]。 |
| In Vivo | Cytarabine(250 mg/kg)也会导致胎盘生长迟缓，并增加胎盘迷路细胞凋亡，在孕期Slc：Wistar大鼠的胎盘迷路区，从治疗后3小时开始增加，并在恢复到对照水平前6小时达到峰值。 48小时，p53蛋白显著增强，p53转录靶基因如p21，cyclinG1和fas和caspase-3活性[3]。Cytarabine对急性白血病非常有效，导致Cytarabine的G1/S阻滞和同步化，并以弱剂量相关的方式增加白血病布朗挪威大鼠的存活时间，表明使用更高剂量的Cytarabine无助于它对人体的抗白血病作用[4]。 |
| Animal Experiment | 怀孕大鼠在妊娠第13天(GD13)腹膜内(ip)注射250mg/kgCytarabine。在本实验条件下，围产儿胎儿先天畸形和生长迟缓检出率较高，但胎儿死亡率并未明显增加。在处理后1，3，6，9，12，24和48小时，在乙醚麻醉下通过心脏穿刺杀死6个水坝，并收集胎盘。作为对照，在GD13上腹膜内注射6只怀孕的大鼠，并在与Cytarabine处理组相同的时间点处死。 |
| Kinase Experiment | 在无水乙醇中制备Cytarabine的储备溶液，并制备Cytarabine的连续稀释液。将CCRF-CEM细胞悬浮于补充有10％FBS，0.1％庆大霉素和1％丙酮酸钠的RPMI培养基中。将细胞悬浮在它们各自的培养基中，得到10mL体积的细胞悬浮液，最终密度为3-6×10 4个细胞/ mL。将适量的Cytarabine溶液转移至细胞悬浮液中，并继续培养72小时。将细胞离心并重新悬浮于不含Cytarabine的新培养基中，并测定最终细胞计数。通过细胞计数与Cytarabine浓度的S形曲线拟合分析数据，结果表示为IC 50(抑制细胞生长的Cytarabine浓度至对照值的50％)。 |
| Data Literature Source | [1]. 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 in sympathetic 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 impaired proliferation 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 with myelocytic leukaemia. Br J Cancer，1988. 58(6): p. 730-3 |
| Unit | Bottle |
| Specification | 50mg 10mM*1mL in Water 100mg 500mg |
Examples of using this product（for reference only）
In Vitro:
Cell（K562 cells；0.1 ng/mL cytarabine；5d）:
K562 cells were cultured in RPMI-1640 medium containing 10% fetal bovine serum and 1% penicillin and streptomycin. K562 cells were differentiated by erythroid induction at an initial concentration of 1×105/mL cells. A final concentration of 40 μM hemin (Solarbio, China) and 0.1 ng/mL cytarabine (Solarbio, China) were added to the medium to induce erythroid differentiation, and the cells were placed at 37℃ under hypoxic (5% CO2, 5% O2), CoCl (200 μM) and normoxic (5% CO2, 20% O2) conditions for 5 days.
Reference：
Gao Z, Li Z, Li X, Xiao J, Li C. Regulation of erythroid differentiation in K562 cells by the EPAS1-IRS2 axis under hypoxic conditions. Front Cell Dev Biol. 2023 Jun 1;11:1161541. doi: 10.3389/fcell.2023.1161541. PMID: 37325570; PMCID: PMC10267359.
In Vivo:
Mice（50~200 mg/kgAra-C，I.P，7d）:
After a week to adapt to the facility, mice were randomly divided into four groups (n = 10 mice per group) for intestinal pathology and survival analysis in the selection of the optimal doses of Ara-C. Ara-C and AS-IV were dissolved by 0.9% saline and dimethyl sulfoxide(DMSO) respectively. The control group was injected intraperitoneally with 0.9% saline (5 ml/kg) and the Ara-C group was intraperitoneally injected with different doses of Ara-C (50 mg/kg, 100 mg/kg, 200 mg/kg) for 7 days. Mice were killed at day 10.
Reference：
Li JJ, Li YL, Chu W, Li GQ, Zhang M, Dong JJ, Li L, Li CH, Zhang JB, Li JW, Jin XJ, Liu YQ. Astragaloside IV alleviates cytarabine-induced intestinal mucositis by remodeling macrophage polarization through AKT signaling. Phytomedicine. 2023 Jan;109:154605. doi: 10.1016/j.phymed.2022.154605. Epub 2022 Dec 15. PMID: 36610133.
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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Li JJ, et al. Phytomedicine. 2023 Jan;109154605.
Li JJ, et al. Phytomedicine. 2023 Jan;109154605.
Gao Z, Li Z, Li X, Xiao J, Li C. Front Cell Dev Biol. 2023 Jun 1;11:1161541.
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