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熔点：300°C
包装规格：2mg 10mg 50mg in glass bottle
溶解性：溶于DMSO(10mg/ml 加热）和水
产品描述：基本信息 产品编号：N80005 产品名称：Nocodazole CAS: 31430-18-9   储存条件 粉末 2-8℃ 四年     分子式： C14H11N3O3S 溶于液体 -80℃ 六个月 分子量 301.32 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 7.5mg/mL (24.89mM) Ethanol Insoluble Water Insoluble 体内（现配现用） 2% DMSO+30% PEG 300+2% Tween 80+ddH2O 1mg/mL ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.3187mL 16.5937mL 33.1873mL 5mM 0.6637mL 3.3187mL 6.6375mL 10mM 0.3319mL 1.6594mL 3.3187mL   生物活性 产品描述 快速可逆的微管聚合抑制剂，也可有效抑制ABL，ABL(E255K) 和 ABL(T315I) 的活性，IC50 值分别为 0.21?μM，0.53?μM 和 0.64?μM。 靶点/IC50 Abl 91nM (Kd) ABL(T315I) 170nM (Kd) EGFR (WT)(Cell-free assay) BRAF 1.8μM (Kd) BRAF(V600E) 1.μM (Kd) c-KIT 1.6μM (Kd) MEK1 1.7μM (Kd) MEK2 1.6μM (Kd) MET 1.7μM (Kd) PI3Kγ 1.5μM (Kd) Microtubule/Tubulin (Kd) CRISPR/Cas9 (Kd)   体外研究 Nocodazole exhibits good affinity toward c-KIT, with a Kd value of 1.6 μM in highly malignant human cancer cells. Nocodazole displays good binding affinity toward the components of the mitogen-activated protein kinase (MAPK) pathway, such as BRAF (Kd=1.8μM), BRAF(V600E) (Kd=1.1μM), MEK1 (Kd=1.7μM), and MEK2 (Kd=1.6μM). Nocodazole has the highest affinity for αβIV and the lowest affinity for αβIII. Nocodazole (1nM) induces apoptosis of COLO 205 cancer cells. Nocodazole (≥ 30µg/mL) significantly increases the percentage of annexin-V-binding cells without significantly modifying average forward scatter of human erythrocytes.   体内研究 Nocodazole (5 mg/kg/three times per week, i.p.)has antitumor effects in athymic mice bearing COLO 205 tumor xenografts.Nocodazole (1nM) + R-41400 dramatically increase the levels of p21/CIP1 and p27/KIP1 protein in the tumor tissues.   推荐实验方法(仅供参考) 细胞实验: Proteins are loaded at 50μg/lane and separated by 12% (w:v) sodium dodecyl sulfate-polyacrylamide gel electrophoresis, blotted, and probed with antibodies for cyclin E, p53, p21/CIP1, p27/KIP1, glyceraldehyde 3-phosphate dehydrogenase (GAPDH), cyclin A, cyclin D1, cyclin D3, cyclin B, CDK2, CDK4, and cytochrome C. Immunoreactive bands are visualized by incubating with the colorigenic substrates nitroblue tetrazolium and 5-bromo-4-chloro-3-indolyl-phosphate. The expression of GAPDH is used as the control for equal protein loading.   动物实验:   COLO 205 cells are grown in RPMI 1640 supplemented with 10% FCS. Cells are harvested through two consecutive trypsinizations, centrifuged at 300×g; for 5 min, washed twice, and resuspended in sterile phosphate-buffered saline (PBS). Cells (5×105 ) in 0.1mL are injected subcutaneously between the scapulae of each nude mouse. After transplantation, tumor size is measured with calipers, and the tumor volume is estimated. Once tumors reach a mean size of 200 mm3 , animals receive intraperitoneal injections of DMSO (25μL), R-41400 (50mg/kg), nocodazole (5mg/kg), or R-41400 + nocodazole three times per week for 6 wk.
保存条件：2-8℃

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