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Talazoparib

产品编号 T6253 CAS 1207456-01-6

别名: LT-673, BMN-673, 他拉唑帕利

Talazoparib (LT-673) 是一种具有口服活性的 PARP 1/2抑制剂，IC50为0.58 nM，具有抗肿瘤活性。它抑制 PARP1 和 PARP2 酶活性的 Ki 值分别为 1.2 nM 和 0.87 nM。

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Talazoparib, CAS 1207456-01-6

规格	价格/CNY	货期
1 mg	￥ 253	现货
2 mg	￥ 357	现货
5 mg	￥ 588	现货
10 mg	￥ 863	现货
25 mg	￥ 1,550	现货
50 mg	￥ 2,580	现货
100 mg	￥ 3,490	现货
200 mg	￥ 4,990	现货
500 mg	￥ 7,790	现货
1 mL * 10 mM (in DMSO)	￥ 659	现货

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其他形式的 Talazoparib:

(8R,9S)-Talazoparib
询价
Talazoparib tosylate
询价

选择批次

纯度: 99.85%

纯度: 99.82%

纯度: 99.69%

纯度: 99.42%

纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1/2 (Kis: 1.2/0.85 nM).
靶点活性	PARP2:0.87 nM (Ki, cell free), PARP1:1.2 nM (Ki, cell free)
体外活性	Talazoparib (BMN 673) demonstrates excellent potency, inhibiting PARP1 and PARP2 enzyme activity with Ki = 1.2 and 0.87 nM, respectively. It inhibits PARP-mediated PARylation in a whole-cell assay with an EC50 of 2.51 nM and prevents the proliferation of cancer cells carrying mutant BRCA1/2, with EC50 = 0.3 nM (MX-1) and 5 nM (Capan-1), respectively [1]. BMN 673 is a potent PARP1/2 inhibitor (PARP1 IC50 = 0.57 nmol/L), but it does not inhibit other enzymes that we have tested. BMN 673 selectively targeted tumor cells with BRCA1, BRCA2, or PTEN gene defects with 20- to more than 200-fold greater potency than existing PARP1/2 inhibitors [2].
体内活性	Talazoparib is orally available, displaying favorable pharmacokinetic (PK) properties and remarkable antitumor efficacy in the BRCA1 mutant MX-1 breast cancer xenograft model following oral administration as a single agent or in combination with chemotherapy agents such as temozolomide and cisplatin [1]. Oral administration of BMN 673 elicited remarkable antitumor activity in vivo; xenografted tumors that carry defects in DNA repair due to BRCA mutations or PTEN deficiency were profoundly sensitive to oral BMN 673 treatment at well-tolerated doses in mice. Synergistic or additive antitumor effects were also found when BMN 673 was combined with temozolomide, SN38, or platinum drugs [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].
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].
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].

别名	LT-673, BMN-673, 他拉唑帕利
化合物与蛋白结合的复合物	Structure of the catalytic domain of tankyrase 1 in complex with talazoparib
分子量	380.35
分子式	C19H14F2N6O
CAS No.	1207456-01-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6292 mL	13.1458 mL	26.2916 mL	65.7289 mL
	5 mM	0.5258 mL	2.6292 mL	5.2583 mL	13.1458 mL
	10 mM	0.2629 mL	1.3146 mL	2.6292 mL	6.5729 mL
	20 mM	0.1315 mL	0.6573 mL	1.3146 mL	3.2864 mL
	50 mM	0.0526 mL	0.2629 mL	0.5258 mL	1.3146 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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容积 (起始)

浓度 (终)

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参考文献

1. Wang B, et al. Molecular Cancer Therapeutics, 2009, 8 (12 Suppl), A121. 2. Shen YQ, et al. Cancer Research, 2010, 70 (8 Suppl), Abstract nr 3514. 3. Kiehlmeier S, Rafiee M R, Bakr A, et al. Identification of therapeutic targets of the hijacked super-enhancer complex in EVI1-rearranged leukemia[J]. Leukemia. 2021: 1-12.

文献引用

1. Hou X, Tian M, Ning J, et al.PARP inhibitor shuts down the global translation of thyroid cancer through promoting Pol II binding to DIMT1 pause.International Journal of Biological Sciences.2023, 19(12): 3970. 2. Mateos-Pujante A, Jiménez M C, Andreu I.Assessment of the PARP inhibitor talazoparib photosafety profile.Biomedicine & Pharmacotherapy.2023, 167: 115593. 3. Kamaletdinova T, Zong W, Urbánek P, et al.Poly (ADP-Ribose) Polymerase-1 Lacking Enzymatic Activity Is Not Compatible with Mouse Development.Cells.2023, 12(16): 2078. 4. Kiehlmeier S, Rafiee M R, Bakr A, et al. Identification of therapeutic targets of the hijacked super-enhancer complex in EVI1-rearranged leukemia. Leukemia. 2021 Nov;35(11):3127-3138. doi: 10.1038/s41375-021-01235-z. Epub 2021 Apr 28.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Talazoparib 1207456-01-6 Chromatin/Epigenetic DNA Damage/DNA Repair PARP inhibit BRCA1/2 LT-673 BMN-673 MX-1 PARP-mediated 他拉唑帕利 poly ADP ribose polymerase LT 673 BMN673 breast cancer Inhibitor PARylation LT673 anticancer BMN 673 inhibitor

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Talazoparib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

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