化合物 Tozasertib|T2509

Tozasertib
639089-54-6

￥348 10mg 起订

￥668 25mg 起订

￥996 50mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 化合物 Tozasertib

英文名称：: Tozasertib

CAS号：: 639089-54-6

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.99%

产品类别：: 抑制剂

货号：: T2509

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.
溶解度	DMSO : 40 mg/mL (86.1 mM)
关键字	VX680 \| inhibit \| Aurora Kinase \| Inhibitor \| VX-680 \| MK0457 \| MK 0457 \| Autophagy \| Tozasertib
相关产品	Guanidine hydrochloride \| Naringin \| Valproic Acid \| Taurine \| Gefitinib \| Aceglutamide \| Hydroxychloroquine \| Curcumin \| Stavudine \| Salicylic acid \| Paeonol \| Sodium 4-phenylbutyrate
相关库	经典已知活性库 \| 抗癌活性化合物库 \| 抗癌上市药物库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 高选择性抑制剂库 \| 药物功能重定位化合物库 \| 酪氨酸激酶分子库 \| FDA 上市激酶抑制剂库 \| 抗癌药物库

VX 680|||MK-0457|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

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