化合物 NMS-P937|T6247|TargetMol

Onvansertib
1034616-18-6

￥233 1mg 起订

￥538 5mg 起订

￥828 10mg 起订

上海更新日期：2024-09-30

TargetMol中国（陶术生物）

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邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 NMS-P937

英文名称：: Onvansertib

CAS号：: 1034616-18-6

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：: 99.88%

产品类别：: 抑制剂

货号：: T6247

Product Introduction

Bioactivity

名称	Onvansertib
描述	Onvansertib (NMS-1286937) is a PLK1 inhibitor (IC50=2 nM) with high selectivity and oral activity. Onvansertib has antitumor activity and inhibits tumor growth.
细胞实验	Cells are seeded into 96- or 384-well plates at densities ranging from 10,000 to 30,000/cm2 for adherent and 100,000/mL for nonadherent cells in appropriate medium supplemented with 10% fetal calf serum. After 24 hours, cells were treated in duplicate with serial dilutions of NMS-P937, and 72 hours later, the viable cell number was assessed by the CellTiter-Glo Assay (Promega). IC50 values were calculated with a sigmoidal fitting algorithm (Assay Explorer MDL). Experiments were carried out independently at least twice.(Only for Reference)
激酶实验	Kinase profile: The inhibitory activity of putative kinase inhibitors and the potency of selected compounds are determined using a trans-phosphorylation assay. Specific peptide or protein substrates are trans-phosphorylated by their specific serine-threonine or tyrosine kinase, in the presence of ATP traced with 33P-γ-ATP, at optimized buffer and cofactors conditions. At the end of the phosphorylation reaction, more than 98% unlabeled ATP and radioactive ATP is captured by adding an excess of the ion exchange dowex resin; the resin then settles down to the bottom of the reaction plate by gravity. Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, followed by evaluation by b-counting. Inhibitory potency evaluation for all the tested kinases was performed at 25 °C using a 60 min end-point assay where the concentrations of ATP and substrates are kept equal to 2 x αKm and saturated (>5 x αKm), respectively.
体外活性	方法: 137 个肿瘤细胞用 Onvansertib 处理 72 h，使用 CellTiter-Glo Assay 检测细胞活力。结果: 137 个细胞系中的 60 个细胞系的 IC50 值低于 100 nmol/L，只有 9 个细胞系的 IC50 值高于 1 µmol/L，表明活性范围广泛。[1] 方法: Cisplatin 敏感和耐药的 CAL33 细胞用 Onvansertib (25-50 nM) 处理 24 天，使用 Flow cytometry 检测细胞周期。结果: Onvansertib 治疗以剂量依赖的方式诱导 G2/M 期所有敏感和耐药 CAL33 细胞的积累。[2]
体内活性	方法: 为检测体内抗肿瘤活性，将 Onvansertib (60 mg/kg) 口服给药给携带 HCT116 异种移植物的 Hsd, athymic nu/nu 小鼠，每天一次，持续八天。结果: Onvansertib 能在最小的体重减轻的情况下获得良好的抗肿瘤活性，在相当程度上抑制了肿瘤生长，TGI 为 79%。[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 : 55 mg/mL (103.28 mM) Ethanol : 10 mg/mL (18.77 mM), Heating is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字	NMS 1286937 \| inhibit \| Inhibitor \| Apoptosis \| NMS-P 937 \| NMS1286937 \| Onvansertib \| Polo-like Kinase (PLK) \| NMS-P-937
相关产品	Lidocaine hydrochloride \| Metronidazole \| 5-Fluorouracil \| Stavudine \| Tributyrin \| Dextran sulfate sodium salt (MW 4500-5500) \| Myricetin \| Sorafenib \| L-Ascorbic acid \| Acetylcysteine \| Sodium 4-phenylbutyrate \| Kaempferol
相关库	抑制剂库 \| 经典已知活性库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 高选择性抑制剂库 \| 抗衰老化合物库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库

NMS-P937|||NMS-1286937|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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员工人数	100-500人
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经营模式	贸易,工厂,试剂,定制,服务
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务