货号:A497931 同义名: 22-Oxovincaleukoblastine sulfate;Leurocristine sulfate
Vincristine sulfate是一种抗肿瘤长春花生物碱,通过抑制有丝分裂纺锤体中微管的形成,使分裂细胞停滞在中期阶段。它与微管结合的Ki值为85 nM。
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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快速发货 顺丰冷链运输,1-2 天到达
品质保证
技术支持
免费溶解
产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SBI-0206965 |
+++
ULK2, IC50: 711 nM ULK1, IC50: 108 nM |
97% | |||||||||||||||||
Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
MRT68921 hydrochloride |
++++
ULK2, IC50: 1.1 nM ULK1, IC50: 2.9 nM |
99%+ | |||||||||||||||||
ROC-325 | ✔ | 99%+ | |||||||||||||||||
Autophinib |
+++
Autophagy, IC50: 40 nM |
97% | |||||||||||||||||
Lys05 | ✔ | 99%+ | |||||||||||||||||
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。 |
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 | ||
A549 | 100 nM | Function Assay | 16 h | leads to a loss of microtubules | 23598276 |
Dose | Dog: 1 mg/kg[3] (i.v.) Monkey: 1 mg/kg - 4 mg/kg[3] (i.v.) Rat: 0.025 mg/kg - 0.5 mg/kg[3] (i.v.) |
Administration | i.v. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 2068-78-2 |
分子式 | C46H58N4O14S |
分子量 | 923.036 |
别名 | 22-Oxovincaleukoblastine sulfate;Leurocristine sulfate;VCR;Oncovin;NSC 67574;Novopharm;Leurocristine;Lilly 37231;Kyocristine;Vincristine (sulfate);NSC-67574 sulfate |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
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 |