Talazoparib tosylate BMN 673ts|cas:1373431-65-2|西域试剂

Talazoparib tosylate BMN 673ts,99.72%

产品编号：Bellancom-108413| CAS NO：1373431-65-2| 分子式：C₂₆H₂₂F₂N₆O₄S| 分子量：552.55

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货号	价格	库存与货期
Bellancom-108413	￥1030.00	杭州北京（现货）
Bellancom-108413	￥1550.00	杭州北京（现货）
Bellancom-108413	￥2450.00	杭州北京（现货）
Bellancom-108413	￥6500.00	杭州北京（现货）
Bellancom-108413	￥11000.00	杭州北京（现货）

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Talazoparib tosylate BMN 673ts

产品介绍

Talazoparib tosylate (BMN 673ts) 是一种新型，高效，有可口服活性的 PARP1/2 抑制剂，抑制PARP1的IC₅₀ 值为 0.57 nM。

生物活性

Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC₅₀ of 0.57 nM for PARP1.

体外研究

Talazoparib is a potent PARP1/2 inhibitor (PARP1 IC₅₀=0.57 nM), it has no effect on PARG activity at concentrations up to 1 μM. Talazoparib binds to PARP1 with a dissociation constant (K_D) of 0.29 nM. Talazoparib inhibits PARP1 and -2 to a similar extent, with K_is of 1.20 and 0.85 nM, respectively. Talazoparib selectively targets tumor cells with BRCA1, BRCA2, or PTEN gene defects with 20- to more than 200-fold greater potency than existing PARP1/2 inhibitors. Talazoparib targets tumor cells with homologous recombination gene defects. Tumor models that are either BRCA1-deficient (MX-1 and SUM149) or BRCA2-deficient (Capan-1) are profoundly sensitive to Talazoparib. Talazoparib induces nuclear γ-H2AX foci at concentrations as low as 100 pM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Talazoparib is readily orally bioavailable, with more than 40% absolute oral bioavailability in rats when dosed in carboxylmethyl cellulose. Oral administration of Talazoparib elicits remarkable antitumor activity; xenografted tumors that carry defects in DNA repair due to BRCA mutations or PTEN deficiency are profoundly sensitive to oral Talazoparib treatment at well-tolerated doses in mice. Synergistic or additive antitumor effects are also found when Talazoparib is combined with temozolomide, SN38, or platinum drugs.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 108 mg/mL (195.46 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8098 mL	9.0490 mL	18.0979 mL
5 mM	0.3620 mL	1.8098 mL	3.6196 mL
10 mM	0.1810 mL	0.9049 mL	1.8098 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 (sealed storage, away from moisture)。-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% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.52 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.52 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。