Vincristine sulfate

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Chemical Structure| 2068-78-2 同义名 : 22-Oxovincaleukoblastine sulfate;Leurocristine sulfate;VCR;Oncovin;NSC 67574;Novopharm;Leurocristine;Lilly 37231;Kyocristine;Vincristine (sulfate);NSC-67574 sulfate
CAS号 : 2068-78-2
货号 : A497931
分子式 : C46H58N4O14S
纯度 : 98+%
分子量 : 923.036
MDL号 : MFCD27980578
存储条件:

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 85 mg/mL(92.09 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: 50 mg/mL(54.17 mM),配合低频超声助溶

动物实验配方:

PO 0.5% CMC-Na 80 mg/mL suspension

生物活性
描述 Leurocristine Sulfate is an inhibitor for polymerization of microtubules with IC50 value of 32μM. It inhibited assembly-end addition with IC50 value of 0.085μM and exhibited 50% cell proliferation inhibition effect shown as >2 fold compared with vinblastine. Besides, the inhibitor could decrease the tumor growth in L-cells with a ratio of 57% compared to non-drug treatment control which could also be potential to inhibit cell proliferation and tumor production in B16 melanoma cells. In HepG2.2.15 and HepG2-HBV1.1 cells, 0.1 μM Leurocristine showed no significant cytotoxicity to both of them. HBV DNA copies were up-regulated by 4 fold and 5.6 fold in the two cells, respectively. Meanwhile, the secretion of HBV DNA copies and the expression of HBV pgRNA were improved. The intracellular HBsAg and HBcAg expression were also increased significantly. Most importantly, Leurocristine at 0.1μM also declined the proliferation rate by 60% in the stable HBV-expressing cell lines while it was 55% in the two cells mentioned above. This compound could also induce cell cycle arrest at S-phase while decrease the numbers of cells at G1/G0 and G2/M phases. SH-SY5Y cells treated with 0.1μM Leurocristine for different time caused decrease of the percentage of G0 /G1 phase cells gradually from 76.26% to 16.46%, while the percentage of G2/M phase cells increased gradually from 20.60% to 72.34%. The percentage of cells at sub-G1 phase increased from 5.75% to 21.25%. These treated SH-SY5Y cells also exhibited distinct changes in the microtubular structure by causing cell cycle arrest at the M phase and time-course premature termination of mitosis .
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A-172 0.1 μM Growth Inhibition Assay 24/72 h inhibits cell growth time dependently 24530235
A2780 Growth Inhibition Assay IC50=3.5 mM 23829203
A549 Growth Inhibition Assay IC50=0.10 ± 0.03 μM 23971075
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.08mL

0.22mL

0.11mL

5.42mL

1.08mL

0.54mL

10.83mL

2.17mL

1.08mL