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Vincristine sulfate

Vincristine sulfate

产品编号 T1270   CAS 2068-78-2
别名: Leurocristine, 22-Oxovincaleukoblastine sulfate, Leurocristine sulfate, 硫酸长春新碱

Vincristine sulfate (Leurocristine sulfate) 是一种抗肿瘤长春花生物碱。在细胞周期的 S 期不可逆地与微管(Ki: 85 nM) 和纺锤体蛋白结合,并干扰有丝分裂纺锤体的形成。

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Vincristine sulfate Chemical Structure
Vincristine sulfate, CAS 2068-78-2
规格 价格/CNY 货期 数量
20 mg ¥ 866 现货
1 mL * 10 mM (in DMSO) ¥ 511 现货
其他形式的 Vincristine sulfate:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Vincristine sulfate (T1270)
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纯度: 99.87%
纯度: 99.35%
纯度: 99.19%
纯度: 98.41%
纯度: 98%
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天然产物信息
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存储 & 溶解度
参考文献
植物来源
结构类型
产品描述 Vincristine sulfate (Leurocristine sulfate) binds irreversibly to microtubules and spindle proteins in S phase and interferes the formation of the mitotic spindle.
靶点活性 Microtubule:85 nM (Ki, cell free)
体外活性 Vincristine 抑制微管蛋白添加(Ki,0.085µg/mL)。在L细胞中,Vincristine 在40纳摩尔浓度下引起约25%的生长抑制[1]。Vincristine 抑制SH-SY5Y细胞增殖呈时间和剂量依赖性(IC50:0.1µg/mL)。0.1µg/mL的VCR诱导细胞进入有丝分裂阻塞和凋亡,促进caspase-3和-9以及cyclin B的表达,同时减少cyclin D在6、12、18和24小时的表达[2]。在体外研究了Vincristine 在0.05mM浓度下对猫迷走神经轴突超微结构的影响。0.1mM的Vincristine 引起微管结构破坏、顺晶结构出现以及神经原纤维的增加[3]。
细胞实验 SH-SY5Y cells at a logarithmic phase were seeded in 96-well plates (at 2x10^6/l) and incubated for 12 h until cells formed a monolayer. Wells were randomly chosen for treatment groups and a control group. For the treatment groups, cells were incubated with 200 μl of cell culture medium containing 0.001, 0.01, 0.1, 1 or 10 μM of VCR. In the control group, cells were grown in 200 μl cell culture medium only. Cells were incubated for another 24, 48 and 72 h and then 20 μl of 5 g/l MTT (0.1 mg/l final concentration) was added to each well. After 4 h of incubation, the cell culture supernatant was removed, 150 μl of DMSO was added to each well and the plate was shaken for 10 min. The absorbance of each well was detected at 490 nm (A value) on an ELISA plate reader. The growth inhibition rate of VCR-treated cells was calculated as: Growth inhibition rate % = [(average A value of control group - average A value of VCR-treated group)/average A value of control group] x 100%. This experiment was performed in triplicates [2].
动物实验 Vincristine (1?mg/ml) was diluted in saline and administered i.v. to wild-type and Mdr1ab/Mrp1 TKO mice, aged 10–14 weeks, at dose levels ranging between 0.125 and 4?mg/kg. Animals were monitored daily and killed when they lost more than 20% of their initial body weight. The MTD was defined as one dose step below the dose where more than one animal in that group had to be killed. Necropsies were performed in wild-type and Mdr1ab/Mrp1 TKO mice receiving vincristine at or near the MTD and killed 2 days later [5].
别名 Leurocristine, 22-Oxovincaleukoblastine sulfate, Leurocristine sulfate, 硫酸长春新碱
分子量 923.04
分子式 C46H58N4O14S
CAS No. 2068-78-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (54.17 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: 92.3 mg/mL(100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 1.0834 mL 5.4169 mL 10.8338 mL 27.0844 mL
5 mM 0.2167 mL 1.0834 mL 2.1668 mL 5.4169 mL
10 mM 0.1083 mL 0.5417 mL 1.0834 mL 2.7084 mL
20 mM 0.0542 mL 0.2708 mL 0.5417 mL 1.3542 mL
50 mM 0.0217 mL 0.1083 mL 0.2167 mL 0.5417 mL
H2O 100 mM 0.0108 mL 0.0542 mL 0.1083 mL 0.2708 mL

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TargetMol Library Books参考文献

1. Jordan, M.A., et al. Comparison of the effects of vinblastine, vincristine, vindesine, and vinepidine on microtubule dynamics and cell proliferation in vitro. Cancer Res, 1985. 45(6): p. 2741-7. 2. Tu Y, et al. Vincristine induces cell cycle arrest and apoptosis in SH-SY5Y human neuroblastoma cells. Int J Mol Med. 2013 Jan;31(1):113-9. 3. Donoso, J.A., et al, Action of the vinca alkaloids vincristine, vinblastine, and desacetyl vinblastine amide on axonal fibrillar organelles in vitro. Cancer Res, 1977. 37(5): p. 1401-7. 4. Baguley, B.C., et al, Inhibition of growth of colon 38 adenocarcinoma by vinblastine and colchicine: evidence for a vascular mechanism. Eur J Cancer, 1991. 27(4): p. 482-7. 5. van Tellingen O, et al. P-glycoprotein and Mrp1 collectively protect the bone marrow from vincristine-induced toxicity in vivo. Br J Cancer. 2003 Nov 3;89(9):1776-82.

TargetMol Library Books文献引用

1. Wang D, Wang Y, Di X, et al.Cortical tension drug screen links mitotic spindle integrity to Rho pathway.Current Biology.2023 2. Hou Z, Ren Y, Zhang X, et al.EP300-ZNF384 transactivates IL3RA to promote the progression of B-cell acute lymphoblastic leukemia.Cell Communication and Signaling.2024, 22(1): 211.
Nirogacestat ZZW-115 hydrochloride Dehydrocrenatidine Staurosporine Diffractaic Acid GW779439X Doxorubicin hydrochloride NVP-TAE 226

相关化合物库

该产品包含在如下化合物库中:
药物功能重定位化合物库 抗癌药物库 抗癌临床化合物库 中药单体化合物库 抗癌上市药物库 微管靶向化合物库 抗癌活性化合物库 天然产物库 高通量筛选天然产物库 共价抑制剂库

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母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Vincristine sulfate 2068-78-2 Apoptosis Cytoskeletal Signaling Microtubule Associated Inhibitor Microtubule/Tubulin NSC-67574 Leurocristine 22-Oxovincaleukoblastine sulfate Vincristine Vincristine Sulfate 22-Oxovincaleukoblastine NSC67574 Leurocristine Sulfate Leurocristine sulfate inhibit NSC 67574 硫酸长春新碱 22-Oxovincaleukoblastine Sulfate inhibitor

 

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