Talazoparib(Synonyms: 他拉唑帕利; BMN-673; LT-673)

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Talazoparib (Synonyms: 他拉唑帕利; BMN-673; LT-673) 纯度: 98.97%

Talazoparib (BMN-673) 是一种高效的，具有口服活性的 PARP 1/2 抑制剂。Talazoparib 抑制 PARP1 和 PARP2 酶活性的 Ki 值分别为 1.2 nM 和 0.87 nM。Talazoparib 具有抗肿瘤活性。

Talazoparib(Synonyms: 他拉唑帕利; BMN-673; LT-673)

Talazoparib Chemical Structure

CAS No. : 1207456-01-6

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生物活性

Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity[1].

IC50 & Target[1]

PARP2

0.87 nM (Ki)

PARP1

1.2 nM (Ki)

体外研究
(In Vitro)

Talazoparib shows an EC50 of 2.51 nM in cellular PARylation assay[1].
Talazoparib shows EC50s of 0.3 nM, 5 nM and 0.31 for MX-1 cells (BRCA1 mutant), Capan-1 cells (BRCA2 mutant) and MRC-5 cells (normal)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Talazoparib (0.33 mg/kg; i.g.; once daily; for 28 days) exhibits antitumor activity against BRCA1 mutant breast cancer model in mice[1].
Talazoparib exhibits moderate oral bioavailability (rat 56%) and Cmax (rat 7948 ng/mL) following oral administration (rat 10 mg/kg)[1]. Talazoparib exhibits the terminal elimination half-life (rat 2.25 h) due to plasma clearance (2 mL/min/kg) following intravenous administration (rat 5 mg/kg)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nu/nu mice (8-10 weeks old), with MX-1 xenograft-bearing mice[1]
Dosage: 0.33 mg/kg
Administration: Oral gavage, once daily, for 28 days
Result: Significantly inhibited xenograft MX-1 tumor growth.
Animal Model: Sprague-Dawley rats[1]
Dosage: 5mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (56%), Cmax (7948 ng/mL), T1/2 (2.25 h).

Clinical Trial

分子量

380.35

Formula

C19H14F2N6O
CAS 号

1207456-01-6
中文名称

他拉唑帕利
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (65.73 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6292 mL 13.1458 mL 26.2916 mL
5 mM 0.5258 mL 2.6292 mL 5.2583 mL
10 mM 0.2629 mL 1.3146 mL 2.6292 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMAC  6% Solutol HS-15   84% PBS

    Solubility: 5 mg/mL (13.15 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.57 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: 1.25 mg/mL (3.29 mM); Suspended solution; Need ultrasonic

  • 4.

    请依序添加每种溶剂： 2% DMSO    40% PEG300    5% Tween-80    53% saline

    Solubility: ≥ 0.5 mg/mL (1.31 mM); Clear solution

  • 5.

    请依序添加每种溶剂： 1% DMSO    99% saline

    Solubility: ≥ 0.25 mg/mL (0.66 mM); Clear solution

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Wang B, et al. Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) Polymerase-1/2 Inhibitor, as an Anticancer Agent. J Med Chem. 2016 Jan 14;59(1):335-57.

    [2]. Shen Y, et al. BMN 673, a novel and highly potent PARP1/2 inhibitor for the treatment of human cancers with DNA repair deficiency.Clin Cancer Res. 2013 Sep 15;19(18):5003-15.

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