Vinblastine sulfate
(Synonyms: 硫酸长春碱; Vincaleukoblastine sulfate salt) 目录号 : GC12286An inhibitor of microtubule assembly
Cas No.:143-67-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Description:
IC50 Value: VIN showed EC50 values of 15 ug/ml, against P815 mastocytoma cells in-vitro[1]. Also supresses nAChR activity with IC50 of 8.9 μM.
Vinblastine can inhibit the formation of microtubule, it also inhibit nAChR. It is a anticancer drug. More and more drug combination was investigated in clinical status.
in vitro: At vinblastine concentrations of 0.5 uM and 2 uM, considerable inhibition of metabolic degradation of vinblastine was observed by competitive inhibitors of CYP3A4 (up to 60% inhibition), 2D6 (30%) and 2E1 (24%), while only a minor effect was observed for 2C9 (14%) and inhibitors of 1A2, 2C8 had no inhibitory effect on vinblastine metabolism. Vinblastine (0.5 and 2 uM) inhibited the metabolic capacity of CYP2C9 (up to 56%), 2C8 (36%), 2D6 (22%) and 3A4-mediated nifedipine oxidation (99%), while 3A4-mediated testosterone 6-beta-hydroxylation (max. 16%) as well as 1A2 and 2E1 remained unaffected[3].
in vivo: In combined intraperitoneal injection with vinblastine (200 micrograms kg-1) into P388/ADR-bearing mice, NA-382 in a suspension form (10 mg kg-1) prolonged the life-span of the mice near to that of P388/S-bearing mice treated with vinblastine alone, but verapamil even at the maximum tolerated dosage (30 mg kg-1) barely affected the in-vivo antitumour effect of vinblastine[2].
Clinical trial: Combination Chemotherapy With or Without Interleukin-2 and Interferon Alfa in Treating Patients With Metastatic Melanoma . Phase 3 Clinical
Cas No. | 143-67-9 | SDF | |
别名 | 硫酸长春碱; Vincaleukoblastine sulfate salt | ||
Canonical SMILES | CCC1(CC2CC(C3=C(CCN(C2)C1)C4=CC=CC=C4N3)(C5=C(C=C6C(=C5)C78CCN9C7C(C=CC9)(C(C(C8N6C)(C(=O)OC)O)OC(=O)C)CC)OC)C(=O)OC)O.OS(=O)(=O)O | ||
分子式 | C46H60N4O13S | 分子量 | 909.05 |
溶解度 | ≥ 28.85 mg/mL in DMSO, ≥ 48.2 mg/mL in Water with ultrasonic | 储存条件 | 4°C, protect from light |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.1 mL | 5.5002 mL | 11.0005 mL |
5 mM | 0.22 mL | 1.1 mL | 2.2001 mL |
10 mM | 0.11 mL | 0.55 mL | 1.1 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。