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AZD 2461

Cat. No. 6060 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent PARP inhibitor; orally bioavailable
化学名： 4-[[4-Fluoro-3-[(4-methoxy-1-piperidinyl)carbonyl]phenyl]methyl]-1(2H)-phthalazinone
纯度： ≥98% (HPLC)
说明书
引用文献
评论
文献 (2)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for AZD 2461

AZD 2461 is a potent PARP inhibitor (IC50 values are 2, 5 and 200 nM for PARP2, PARP1 and PARP3, respectively). Exhibits anticancer effects in BRCA1 mutant, but not wild-type breast cancer cell lines in vitro. Inhibits growth of olaparib-resistant mammary tumors in a mouse model and is a poor substrate for the P-gp transporter. Orally bioavailable.

化合物库 for AZD 2461

AZD 2461 is also offered as part of the Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。

技术数据 for AZD 2461

分子量 395.43
公式 C22H22FN3O3
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1174043-16-3
PubChem ID 44199317
InChI Key HYNBNUYQTQIHJK-UHFFFAOYSA-N
Smiles COC1CCN(C(C2=C(C=CC(CC3=NNC(C4=CC=CC=C34)=O)=C2)F)=O)CC1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for AZD 2461

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 39.54 100
ethanol 39.54 100

制备储备液 for AZD 2461

以下数据基于产品分子量 395.43。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.53 mL 12.64 mL 25.29 mL
5 mM 0.51 mL 2.53 mL 5.06 mL
10 mM 0.25 mL 1.26 mL 2.53 mL
50 mM 0.05 mL 0.25 mL 0.51 mL

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参考文献 for AZD 2461

参考文献是支持产品生物活性的出版物。

Oplustil O'Connor et al (2016) The PARP inhibitor AZD2461 provides insights into the role of PARP3 inhibition for both synthetic lethality and tolerability with chemotherapy in preclinical models. Cancer Res. 76 6084 PMID: 27550455

Jaspers et al (2013) Loss of 53BP1 causes PARP inhibitor resistance in Brca1-mutated mouse mammary tumors. Cancer Discov. 3 68 PMID: 23103855

If you know of a relevant reference for AZD 2461, please let us know.

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关键词: AZD 2461, AZD 2461 supplier, AZD2461, potent, PARP, inhibitors, inhibits, poly, (ADP-ribose), polymerases, orally, bioavailable, chemotherapeutics, Poly(ADP-ribose), Polymerase, 6060, Tocris Bioscience

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