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- CAS号：
639089-54-6
- 规格：
1mLx10mM(inDMSO)/2mg/5mg/10mg/25mg/50mg/100mg/500mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥174.0 |
|---|---|---|---|
| 规格： | 2mg | 产品价格： | ￥118.0 |
| 规格： | 5mg | 产品价格： | ￥170.0 |
| 规格： | 10mg | 产品价格： | ￥234.0 |
| 规格： | 25mg | 产品价格： | ￥420.0 |
| 规格： | 50mg | 产品价格： | ￥629.0 |
| 规格： | 100mg | 产品价格： | ￥856.0 |
| 规格： | 500mg | 产品价格： | ￥2072.0 |
Product Introduction
Bioactivity
| 名称 | Tozasertib |
| 描述 | Tozasertib (MK-0457) is a pan-Aurora kinase inhibitor (Kis: 0.6/18/4.6 nM for Aurora A/Aurora B/Aurora C). It shows selectivity against more than 190 different kinases. |
| 细胞实验 | Logarithmically growing MCF-7 cells were incubated with either VX-680 or DMSO for 48 h. Single-cell suspensions were fixed in 70% ethanol for 15 min, incubated with RNase (1 mg/ml) at 37 °C for 30 min, labeled with 400 μl propidium iodide (50 μg/ml) for at least 15 min at room temperature. Cell-cycle profiles were determined by flow cytometric analysis [1]. |
| 激酶实验 | Recombinant Aurora-1 (62-344), Aurora-2 (1-403) and Aurora-3 (1-309) were expressed as N-terminal, His6-tagged fusion proteins using a baculovirus expression system. The proteins were purified by affinity chromatography using Ni-NTA agarose, followed by size exclusion using a Superdex 200 26/60 column. Inhibition of kinase activity was assessed using a standard enzyme-coupled system or a radiometric, phosphocellulose-peptide capture assay as previously described [1]. |
| 动物实验 | For the HL-60 study, female athymic NCr-nu mice were inoculated subcutaneously with 10^7 HL-60(TB) leukemia cells into the right axillary area. Treatment was administered i.p. b.i.d. after tumors reached 150–200 mm^3. VX-680 was prepared in a vehicle of 50% PEG 300 in 50 mM phosphate buffer. Cisplatin, formulated in saline, was administered i.p. q.4.d. for a total of three injections, at a dose of 5.4 mg/kg. For the MIA PaCa-2 studies, female MF1 nude mice were inoculated with 10^7 MIA PaCa-2 cells into the dorsal flank. Treatment was administered i.p. b.i.d. after tumors reached 175 mm^3. VX-680 was prepared in a vehicle of 50% PEG 300 in 50 mM phosphate buffer. 5-fluorouracil, formulated in saline, was administered i.v. q.4.d. at a dose of 50 mg/kg. For the HCT116 study, female Hsd RH rnu/nu rats were inoculated with 10^7 HCT116 cells into the right flank. Treatment was administered once the tumors reached 700–950mm^3. VX-680 was administered continuously through an indwelling femoral catheter, followed by a saline infusion for 4 d before repeating the dose cycle. For all studies, tumor volume was determined by caliper measurements three times a week [1]. |
| 体外活性 | Tozasertib (VX-680) 是三种Aurora激酶的强效抑制剂，其表观抑制常数（Ki（app））分别为Aurora-A、Aurora-B和Aurora-C的0.6、18及4.6 nM。VX-680导致细胞聚集在4N DNA含量处，并强力抑制了多种肿瘤细胞类型的增殖，IC50值在15至113 nM之间[1]。不同的甲状腺癌细胞（ATC细胞）经VX-680处理后，其增殖在时间和剂量上表现出依赖性抑制，IC50值在25至150 nM之间。VX-680显著阻碍了不同细胞系在软琼脂中形成菌落的能力。通过对半胱天冬酶-3活性的分析表明，VX-680在不同细胞系中诱导了凋亡[2]。 |
| 体内活性 | 在裸鼠体内，用Tozasertib以每日两次，每次75 mg/kg的剂量通过腹腔注射(b.i.d. i.p.)治疗13天后，与对照组相比，平均肿瘤体积减少了98%。在十只动物中有四只的最终肿瘤体积比治疗前的初始体积还要小。肿瘤生长的减少与剂量成正比，且在12.5 mg/kg b.i.d.剂量下显著。Tozasertib具有良好的耐受性，仅在最高剂量下观察到体重轻微下降（75 mg/kg b.i.d.时，体重下降5%）。Tozasertib还在胰腺和结肠异种移植模型中诱导肿瘤退缩。在一个确立的人类胰腺(MIA PaCa-2)异种移植模型中，用Tozasertib以每日两次，每次50 mg/kg通过腹腔注射(b.i.d i.p.)治疗，使得十个肿瘤中有七个出现退缩，并且与治疗前的初始肿瘤体积相比，平均肿瘤体积减少了22% [1]。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+90% Saline : < 10 mg/mL (21.52 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (21.52 mM), Suspension. DMSO : 122.5 mg/mL (263.67 mM), Sonication is recommended. |
| 关键字 | VX-680 | VX680 | Tozasertib | MK0457 | MK 0457 | Inhibitor | inhibit | Autophagy | AuroraKinase | Aurora Kinase | Aurora C | Aurora B | Aurora A |
| 相关产品 | Guanidine hydrochloride | Naringin | Enzalutamide | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Hemin | Hydroxychloroquine | Sildenafil citrate | Stavudine | Tamoxifen | Paeonol |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Anti-Aging Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 Tozasertib【639089-54-6】
￥118 - 2072
