Ambeed.cn

首页 / / / PARP / Talazoparib

他拉唑帕利 /Talazoparib {[allProObj[0].p_purity_real_show]}

货号:A570059 同义名: BMN-673;LT-673

Talazoparib (BMN-673) 是一种高效、口服活性的PARP1/2抑制剂,对PARP1PARP2的Ki值分别为1.2 nM和0.87 nM。它具有抗肿瘤活性。

Talazoparib 化学结构 CAS号:1207456-01-6
Talazoparib 化学结构
CAS号:1207456-01-6
Talazoparib 3D分子结构
CAS号:1207456-01-6
Talazoparib 化学结构 CAS号:1207456-01-6
Talazoparib 3D分子结构 CAS号:1207456-01-6
规格 价格 会员价 库存 数量
{[ item.pr_size ]}

{[ getRatePrice(item.pr_rmb, 1,1) ]}

{[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]}

{[ getRatePrice(item.pr_rmb, 1,1) ]}

{[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]}
{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_am, item.pr_size) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} 现货 咨询 - +
购物车0 收藏 询单

Talazoparib 纯度/质量文件 产品仅供科研

货号:A570059 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

全球学术期刊中引用的产品

Cell Host Microbe, 2024. Ambeed. [ A163338 ]
Cancer Res., 2024. Ambeed. [ A295334 ]
J. Pharm. Investig., 2024. Ambeed. [ A221527 , A691302 , A272538 , A187261 ]
J. Fungi, 2024, 10(11): 751. Ambeed. [ A796919 ]
JBC, 2024, 107935. Ambeed. [ A194396 ]
更多 >
产品名称 PARP PARP1 PARP2 PARP3 其他靶点 纯度
PJ34 HCl ++

PARP, EC50: 20 nM

99%+
Rucaparib phosphate ++++

PARP, Ki: 1.4 nM

99%+
3-Aminobenzamide ++

PARP, IC50: <50 nM

98%
AZD-2461 99%+
BGP-15 99%+
NU1025 +

PARP, IC50: 400 nM

97%
Benzamide +

PARP, IC50: 3.3 μM

98%
Picolinamide +

PARP, IC50: 95 μM

98%
AG14361 +++

PARP1, Ki: <5 nM

98+%
Iniparib 98%
Talazoparib ++++

PARP1, IC50: 0.57 nM

99%+
NMS-P118 ++

PARP1, Kd: 0.009 μM

98+%
UPF 1069 +

PARP1, IC50: 8.0 μM

++

PARP2, IC50: 0.3 μM

98%
A-966492 ++++

PARP1, Ki: 1 nM

PARP1, EC50: 1 nM

+++

PARP2, Ki: 1.5 nM

99%+
Veliparib ++

PARP1, Ki: 5.2 nM

+++

PARP2, Ki: 2.9 nM

98%
Niraparib tosylate +++

PARP1, IC50: 3.8 nM

+++

PARP2, IC50: 2.1 nM

99%+
Stenoparib ++++

PARP1, IC50: 1 nM

++++

PARP2, IC50: 1.2 nM

98%
Olaparib +++

PARP1, IC50: 5 nM

++++

PARP2, IC50: 1 nM

98%
Niraparib +++

PARP1, IC50: 3.8 nM

+++

PARP2, IC50: 2.1 nM

98%
ME0328 +

PARP1, IC50: 6.3 μM

+

PARP3, IC50: 0.89 μM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Talazoparib 生物活性

靶点
  • PARP1

    PARP1, IC50:0.57 nM

描述 PARP1, also called as Poly(ADP-ribose) polymerase, is involved in the signaling of DNA damage. It can recognize and bind DNA single or double-strand breaks, thus possessing various cellular function, including regulation of apoptosis and chromosome stability, gene amplification and transcription, as well as cell division and differentiation. PARP-2 is the closest homolog of PARP1 (~62% similarity in catalytic domain) and compensates for PARP-1 activity in DNA single-strand break. BMN 673 is a potent PARP1/2 inhibitor with IC50 value of 0.57nM for PARP1 (measured by PARP1 enzyme activity). BMN673 showed EC50 value of 2.5nM for inhibition of cellular PAR synthesis in LoVo cells, IC50 value of 5nM for single-agent cytotoxicity of Capan-1 cell survival reduction and GI50 value of 3nM for Temozolomide potentiation assay in LoVo cells. BMN 673 selectivity inhibited BRCA-deficient cells and delivered a therapeutic window between BRCA-proficient and –deficient models at much lower concentrations compared with the other PARP inhibitor, veliparib, rucaparib and olaparib. BMN 673 possessed good pharmacodynamics, as a single oral administration of 1 mg/kg BMN 673 caused drastically decreased intratumoral PAR levels at 2 and 8 hours following drug administration with partial recovery observed at 24 hours after dosing. Oral administration of BMN 673 at dose of 0.33mg/kg, daily, for 28 days caused significant growth inhibition of MX-1 xenografts in mice[1]. BMN 673 showed ~100-fold more potent at trapping PARP-DNA complexes and more cytotoxic as single agent than olaparib[2].
作用机制 BMN 673 is anchored to the nicotinamide-binding pocket of PARP and extends the binding interactions towards the outer edges of the pocket, which exhibit the least sequence homology among PARP enzymes.[3]

Talazoparib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
BR5FVB1-Akt 0.1-100 nM Growth Inhibition Assay 24/48/72 h inhibits cell proliferation dose dependently 26047697
BR5FVB1-Akt 0.1-100 nM Apoptosis Assay 72 h induces apoptosis 26047697
BT-12 Growth Inhibition Assay IC50> 1,000 nM 25263539
Capan-1 Growth Inhibition Assay IC50=16.0 ± 5.4 µM  25864590

Talazoparib 动物研究

Dose Nude Mice: o.1 mg/kg, 0.33 mg/kg[1] (p.o.)
Administration p.o.

Talazoparib 参考文献

[1]Shen Y, Rehman FL, 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.

[2]Murai J, Huang SY, et al. Stereospecific PARP trapping by BMN 673 and comparison with olaparib and rucaparib. Mol Cancer Ther. 2014 Feb;13(2):433-43.

[3]Aoyagi-Scharber M, Gardberg AS, et al. Structural basis for the inhibition of poly(ADP-ribose) polymerases 1 and 2 by BMN 673, a potent inhibitor derived from dihydropyridophthalazinone. Acta Crystallogr F Struct Biol Commun. 2014 Sep;70(Pt 9):1143-9.

Talazoparib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.15mL

2.63mL

1.31mL

26.29mL

5.26mL

2.63mL

Talazoparib 技术信息

CAS号1207456-01-6
分子式C19H14F2N6O
分子量 380.35
别名 BMN-673;LT-673
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 25 mg/mL(65.73 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 45 mg/mL suspension

Ambeed 相关网站 Ambeed.cn Ambeed.com
Ambeed
关于我们
联系我们
资讯中心
网站地图
产品手册
  • 批次文件查询
  • 客户支持
    技术支持
    专业术语
    缩略词释义
    质量手册
    产品咨询
    计算器
    活动政策
    订购方法
    积分商城
    活动声明
    联系我们
    400-920-2911 sales@ambeed.cn tech@ambeed.cn
    Ambeed 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务,不为任何个人或者非科研性质用途提供服务。