![Talazoparib tosylate, 聚[ADP-核糖]聚合酶-1 抑制剂](https://www.aladdin-e.com/media/catalog/product/cache/207e23213cf636ccdef205098cf3c8a3/T/6/T655529.jpg)
计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
干燥,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC 50 of 0.57 nM for PARP1 .
In Vitro
Talazoparib is a potent PARP1/2 inhibitor (PARP1 IC 50 =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 i s 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:IC50: 0.57 nM (PARP1)
规格
别名
甲磺酸他拉唑帕尼
规格或纯度
10mM in DMSO
英文名称
Talazoparib tosylate
生化机理
Talazoparib tosylate (BMN 673ts)是一种新型、强效的口服PARP1/2抑制剂，对PARP1的IC 50为0.57 nM。
储存条件
干燥,-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
聚[ADP-核糖]聚合酶-1 抑制剂
名称和识别符
EC号
806-564-1
分子类型
小分子
Isomeric SMILES
CC1=CC=C(C=C1)S(=O)(=O)O.CN1C(=NC=N1)[C@@H]2[C@H](NC3=CC(=CC4=C3C2=NNC4=O)F)C5=CC=C(C=C5)F
PubChem CID
分子量
552.55
技术文档
高级数据
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C、干燥条件下保存。请与干燥剂一同密封保存，本品对湿气敏感。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 1373431-65-2，分子式为 C26H22F2N6O4S，分子量为 552.55 g/mol。
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每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
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