他拉唑帕利|T6253

Talazoparib
1207456-01-6

￥253 1mg 起订

￥357 2mg 起订

￥588 5mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

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邮箱：marketing@targetmol.com

产品详情:

中文名称：: 他拉唑帕利

英文名称：: Talazoparib

CAS号：: 1207456-01-6

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：: 99.85%

产品类别：: 抑制剂

货号：: T6253

Product Introduction

Bioactivity

名称	Talazoparib
描述	Talazoparib (LT-673) is a PARP inhibitor that inhibits PARP 1 and PARP 2 (Ki=1.2/0.87 nM) and is orally active. Talazoparib has anti-tumorigenic activity and induces tumor cell death by blocking PARP enzyme activity and by trapping PARP at DNA damage sites.
细胞实验	Colony formation assays were conducted as described previously. In brief, cells were seeded into 6-well plates at a concentration of 500 to 2,000 cells per well. After 24 hours, media was replaced with fresh media containing PARP1/2 inhibitor. This procedure was repeated twice weekly for 14 days, at which point colonies were fixed with TCA and stained with sulforhodamine B. Colonies were counted and surviving fractions calculated by normalizing colony counts to colony numbers in vehicle-treated wells. Survival curves were plotted using a four-parameter logistic regression curve fit [2].
激酶实验	The ability of a test compound to inhibit PARP1 enzyme activity was assessed using the PARP Assay Kit following the manufacturer's instruction. IC50 values were calculated using GraphPad Prism5 software. For PARP inhibitor Ki determination, enzyme assays were conducted in 96-well FlashPlate with 0.5 U PARP1 enzyme, 0.25× activated DNA, 0.2 μCi [3H] NAD, and 5 μmol/L cold NAD in a final volume of 50 μL reaction buffer containing 10% glycerol (v/v), 25 mmol/L HEPES, 12.5 mmol/L MgCl2, 50 mmol/L KCl, 1 mmol/L dithiothreitol (DTT), and 0.01% NP-40 (v/v), pH 7.6. Reactions were initiated by adding NAD to the PARP reaction mixture with or without inhibitors and incubated for 1 minute at room temperature. Fifty microliter of ice-cold 20% trichloroacetic acid (TCA) was then added to each well to stop the reaction. The plate was sealed and shaken for a further 120 minutes at room temperature, followed by centrifugation. Radioactive signal bound to the FlashPlate was determined using TopCount. PARP1 Km was determined using Michaelis–Menten equation from various substrate concentrations (1–100 μmol/L NAD). Compound Ki was calculated from enzyme inhibition curve according to the formula: Ki = IC50/[1+(substrate)/Km]. Km for PARP2 enzyme and compound Ki were determined with the same assay protocol except 30 ng PARP2, 0.25× activated DNA, 0.2 μCi [3H] NAD, and 20 μmol/L cold NAD were used in the reaction for 30 minutes at room temperature [2].
动物实验	Female athymic nu/nu mice (8–10-week old) were used for all in vivo xenograft studies. Mice were quarantined for at least 1 week before experimental manipulation. Exponentially growing cells (LNcap and MDA-MB-468) or in vivo passaged tumor fragments (MX-1) were implanted subcutaneously at the right flank of nude mice. When tumors reached an average volume of approximately 150 mm^3, mice were randomized into various treatment groups (6–8 mice/group) in each study. Mice were visually observed daily and tumors were measured twice weekly by calliper to determine tumor volume using the formula [length/2] × [width^2]. Group median tumor volume (mm^3) was graphed over time to monitor tumor growth. In single-agent studies, olaparib (100 mg/kg), BMN 673 (various doses as indicated), or vehicle (10% DMAc, 6% Solutol, and 84% PBS) was administered by oral gavage (per os), once daily or BMN 673 (0.165 mg/kg) twice daily for 28 consecutive days. Mice were continuously monitored for 10 more days after last day of dosing. In cisplatin combination study, BMN 673, olaparib, or vehicle was administered per os once daily for 8 days starting on day 1. Cisplatin at a dosage of 6 mg/kg or its vehicle (saline) was administered intraperitoneally as a single injection on day 3, 30 minutes after PARP inhibitor was administered. Combination with carboplatin was conducted in a similar way in MX-1 model in which BMN 673 was administered per os once daily for either 8 days or 5 days and carboplatin was injected intraperitoneally at single dose of 35 mg/kg, 30 minutes after BMN 673 on day 3 [2].
体外活性	方法：12 种 OCCC 细胞系用 Talazoparib (0-100 nM) 处理 14 天，使用 colony formation assays 检测化合物敏感性。结果：除 KOC-7c 外，所有 HR 缺陷细胞系对 Talazoparib 均显示出具有敏感性的剂量反应曲线。而所有 HR 活性细胞系 (OVTOKO除外) 均显示具有耐药性的剂量响应曲线。[1] 方法：人结肠癌细胞 LoVo 用 Talazoparib (10-40 nM) 和 temozolomide (0-400 µM) 处理 5 天，使用 CellTiterGlo assay 检测细胞活力。结果：单剂 Talazoparib 暴露导致约 15% 的细胞生长抑制。将 temozolomide 与 Talazoparib 组合可显著增强 temozolomide 的细胞毒性。[2]
体内活性	方法：为测试体内抗肿瘤活性，将 Talazoparib (0.166-0.33 mg/kg) 口服给药给携带人乳腺癌肿瘤 MX-1 的 athymic nu/nu 小鼠，每天一次或每天两次，持续四周。结果：Talazoparib 在小鼠异种移植物模型中以 0.165 mg/kg 剂量每天两次给药比 0.33 mg/kg 剂量每天一次给药更有效。在 MX-1 模型中，不仅用 0.165 mg/kg/dose 2X/天方案治疗的所有 6 只小鼠都达到了完全反应，而且直到研究结束，即给药停止 8 周后，没有一只小鼠出现肿瘤再生长。[2]
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 : 36 mg/mL (94.6 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+90% Saline : 0.1 mg/mL (0.26 mM), Working solution is recommended to be prepared and used immediately.
关键字	inhibit \| Talazoparib \| BRCA1/2 \| MX-1 \| PARP-mediated \| poly ADP ribose polymerase \| LT 673 \| BMN673 \| breast cancer \| Inhibitor \| PARylation \| LT673 \| anticancer \| BMN 673 \| PARP
相关产品	VPC-70063 \| Niraparib \| XAV-939 \| Olaparib \| 3-Aminobenzamide \| Benzamide \| OUL35 \| 3-Methoxybenzamide \| 4'-Methoxychalcone \| EB-47
相关库	抑制剂库 \| 抗癌上市药物库 \| 经典已知活性库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| EMA 上市药物库 \| 抗衰老化合物库 \| FDA 上市药物库 \| 抗癌临床化合物库 \| 抗癌药物库

LT-673|||BMN-673|||他拉唑帕利|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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