Ancitabine hydrochloride
作者：齊岳
發(fā)布時間：2023-09-11
09:07:30
點擊數(shù)：
產(chǎn)品名稱：Ancitabine hydrochloride
產(chǎn)品描述：
| 植物來源 | 天然產(chǎn)物 > 其他（植物來源） > 其他 |
| 產(chǎn)品描述 | Ancitabine Hydrochloride is the hydrochloride salt of a cytarabine congener prodrug with antineoplastic activity. Upon administration, ancitabine is slowly hydrolyzed into cytarabine. Subsequently, cytarabine is converted to the triphosphate form within the cell and then competes with cytidine for incorporation into DNA. Because the arabinose sugar sterically hinders the rotation of the molecule within DNA, DNA replication ceases, specifically during the S phase of the cell cycle. Cytarabine agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. Compared to cytarabine, a more prolonged, consistent cytarabine-mediated therapeutic effect may be achieved with ancitabine because of the slow hydrolytic conversion of ancitabine to cytarabine. |
| 體外活性 | 作為一種有效的免疫抑制劑,抗病毒和抗劑,Cyclocytidine可用于白血病**.其需要用不同的復(fù)合注射方法才可發(fā)揮大抑制效果. |
| 體內(nèi)活性 | Cyclocytidine對需要DNA復(fù)制和處于有絲分裂快速分裂期的細(xì)胞作用為明顯。Cyclocytidine對DNA合成所需的DNA和RNA聚合酶以及核苷酸還原酶有也抑制作用。與人類的脫氧核苷結(jié)構(gòu)相似,Cyclocytidine HCl (Ancitabine)整合到人類的DNA以殺死細(xì)胞,是Cytarabine的前體藥物。 |
| 激酶實驗 | Human placental aromatase activity: The assay is performed in a total volume of 1 mL at 37 ℃. Unless otherwise noted, the incubation mixture contains 11 nM [4- 14C] androstene-3, 17-dione ([4- 14C]A), 24 mM NADPH (tetrasodium salt Type III), the appropriate concentrations of the desired inhibitor, and 120 μg of microsomal protein. The (4- 14C)A is added as a solution in 1.7% ethanol in 0.05 M potassium phosphate buffer (pH 7.4), so that the final concentration of ethanol does not exceed 0.02% (v/v). The reaction is started by the addition of enzyme and stopped after 20 min by the addition of 7 vol of ethyl acetate. The mixture is agitated on a vortex mixer and centrifuged at 600 g for 5 min. The aqueous phase is re-extracted with 7 vol of ethyl acetate, and the combined extracts are evaporated to dryness using an Evapo-Mix. Over 99% of the radio- active of [4- 14C] added is recovered using this extraction system. The residue obtained is dissolved in 150 μL acetone, and 100 μL aliquots are chromatographed for 65 min on thin-layer plates precoated with silica gel 60 using ethyl: acetate: isooctane (140:60, v/v; system A) or toluene: chloroform: methanol (70:140:20; system B). The radioactive zones of the plate are located with a Berthold LB 2760 thin-layer scanner. The radioactive estradiol (E2) and estrone (E1) neaks are identified by comparison with authentic standards. The corresponding bonding band of silica gel is transferred to vials containing 10 mL of scintillation fluid, and counted with a 6880 Liquid Scintillation system. |
| 別名 | 環(huán)胞苷, Cyclocytidine hydrochloride, Cyclocytidine HCl, NSC 145668 HCl, Cyclo-CMP hydrochloride, Cyclo-C |
| 分子量 | 261.66 |
| 分子式 | C9H12ClN3O4 |
| CAS No. | 10212-25-6 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: <1 mg/mL
DMSO: 10 mg/mL (38.22 mM)
H2O: 40 mg/mL (152.9 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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