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

目录号: HY-16106 纯度: 99.64%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

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 K_i 值分别为 1.2 nM 和 0.87 nM。Talazoparib 具有抗肿瘤活性。

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Talazoparib Chemical Structure

CAS No. : 1207456-01-6

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1297	In-stock
5 mg	￥1550	In-stock
10 mg	￥2450	In-stock
50 mg	￥3200	In-stock
100 mg	￥5100	In-stock
200 mg	现货	询价
500 mg		询价
1 g		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Talazoparib:

MCE 顾客使用本产品发表的 69 篇科研文献

: Talazoparib purchased from MCE. Usage Cited in: EBioMedicine. 2020 Sep;59:102923. [Abstract]; Western Blot analyses of TP53, p21 and RAD51 in PARP inhibitor sensitive (SKCO1 and LS513) and resistant cell lines (SW1222 and SNU61) after treatment with Talazoparib for 48 h. Talazoparib decreases RAD51 protein expression in the two TP53 wild-type cell lines SKCO1 and LS513.

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

生物活性
纯度 & 产品资料
参考文献

生物活性

Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with K_is 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)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CAPAN-1	IC₅₀	1.8 nM Compound: 5; BMN-673	Antiproliferative activity against human Capan1 cells after 7 days by CCK8 or SRB assay Antiproliferative activity against human Capan1 cells after 7 days by CCK8 or SRB assay	[PMID: 28692916]
DLD-1	IC₅₀	0.002 μM Compound: 4	Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days	[PMID: 34570508]
LoVo	EC₅₀	2.5 nM Compound: 9, BMN 673	Inhibition of PARP in human LoVo cells assessed as inhibition of hydrogen peroxide-induced PARylation treated for 30 mins prior to incubation with H2O2 for 5 mins by fluorescence analysis Inhibition of PARP in human LoVo cells assessed as inhibition of hydrogen peroxide-induced PARylation treated for 30 mins prior to incubation with H2O2 for 5 mins by fluorescence analysis	[PMID: 25761096]
LoVo	EC₅₀	2.51 nM Compound: (8S,9R)-47; BMN 673; Talazoparib	Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay	[PMID: 26652717]
LoVo	GI₅₀	4 nM Compound: (8S,9R)-47; BMN 673; Talazoparib	Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay	[PMID: 26652717]
MDA-MB-436	IC₅₀	0.012 nM Compound: 2; BMN-673	Cytotoxicity against human MDA-MB-436 cells assessed as inhibition of cell viability incubated for 14 days with three intermittent intervals by CellTiterGlo luminescence assay Cytotoxicity against human MDA-MB-436 cells assessed as inhibition of cell viability incubated for 14 days with three intermittent intervals by CellTiterGlo luminescence assay	[PMID: 33120078]
MDA-MB-436	IC₅₀	0.38 nM Compound: 2; BMN-673	Cytotoxicity against human MDA-MB-436 cells assessed as inhibition of cell viability incubated for 4 days by CellTiterGlo luminescence assay Cytotoxicity against human MDA-MB-436 cells assessed as inhibition of cell viability incubated for 4 days by CellTiterGlo luminescence assay	[PMID: 33120078]
MDA-MB-436	IC₅₀	0.7 nM Compound: 5; BMN-673	Antiproliferative activity against human MDA-MB-436 cells after 7 days by CCK8 or SRB assay Antiproliferative activity against human MDA-MB-436 cells after 7 days by CCK8 or SRB assay	[PMID: 28692916]
SUM149PT	EC₅₀	1.6 nM Compound: Talazoparib	Cytotoxicity against BRCA1-deficient human SUM149 cells measured after 6 days by microscopic analysis Cytotoxicity against BRCA1-deficient human SUM149 cells measured after 6 days by microscopic analysis	[PMID: 31042381]
SUM149PT	EC₅₀	23.2 nM Compound: Talazoparib	Cytotoxicity against BRCA1-proficient human SUM149 cells measured after 6 days by microscopic analysis Cytotoxicity against BRCA1-proficient human SUM149 cells measured after 6 days by microscopic analysis	[PMID: 31042381]
V79	IC₅₀	5011.4 nM Compound: 5; BMN-673	Cytotoxicity against BRCA2 expressing Chinese hamster V79 cells after 3 days by CCK8 or SRB assay Cytotoxicity against BRCA2 expressing Chinese hamster V79 cells after 3 days by CCK8 or SRB assay	[PMID: 28692916]

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].

MCE 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 C_max (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].

MCE 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%), C_max (7948 ng/mL), T_1/2 (2.25 h).

Clinical Trial

分子量

380.35

Formula

C₁₉H₁₄F₂N₆O

CAS 号

1207456-01-6

性状

固体

颜色

White to off-white

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	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : 25 mg/mL (65.73 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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

查看完整储备液配制表

* 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

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); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

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); 悬浊液; 超声助溶
方案三

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); 澄清溶液
方案四

请依序添加每种溶剂： 1% DMSO 99% Saline
Solubility: ≥ 0.25 mg/mL (0.66 mM); 澄清溶液

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。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。

方案一

请依序添加每种溶剂： 10% DMAc 6% Solutol HS-15 84% PBS
Solubility: 5 mg/mL (13.15 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.89%

选择批次：

Data Sheet (630 KB) SDS (393 KB)

COA (292 KB) LCMS (125 KB) 元素分析报告 (215 KB)

产品使用指南 (1538 KB)

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. [Content Brief]

[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. [Content Brief]

Talazoparib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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
	15 mM	0.1753 mL	0.8764 mL	1.7528 mL	4.3819 mL
	20 mM	0.1315 mL	0.6573 mL	1.3146 mL	3.2864 mL
	25 mM	0.1052 mL	0.5258 mL	1.0517 mL	2.6292 mL
	30 mM	0.0876 mL	0.4382 mL	0.8764 mL	2.1910 mL
	40 mM	0.0657 mL	0.3286 mL	0.6573 mL	1.6432 mL
	50 mM	0.0526 mL	0.2629 mL	0.5258 mL	1.3146 mL
	60 mM	0.0438 mL	0.2191 mL	0.4382 mL	1.0955 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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

Customer Review

Other Forms of Talazoparib:

MCE 顾客使用本产品发表的 69 篇科研文献

Talazoparib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 PARP 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

Talazoparib 相关分类

完整储备液配制表

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

Customer Review

Other Forms of Talazoparib:

Talazoparib 相关抗体

MCE 顾客使用本产品发表的 69 篇科研文献

Talazoparib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 PARP 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

Talazoparib 相关抗体:

摩尔计算器

稀释计算器

Talazoparib 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

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