Pamiparib|1446261-44-4|(BGB-290)-陌孚医药/Medlife

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Pamiparib (Synonyms: BGB-290)

目录号: PL08910 纯度: ≥99%

CAS No. :1446261-44-4

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中文名称	Pamiparib
中文别名	(R)-2-fluoro-10a-methyl-7,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(5H)-one
英文名称	Pamiparib
英文别名	(R)-2-fluoro-10a-methyl-7,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(5H)-one;Pamiparib;8375F9S90C;Pamiparib [INN];Pamiparib [USAN];Pamiparib (USAN/INN);Pamiparib [USAN:INN];BGB290;DENYZIUJOTUUNY-MRXNPFEDSA-N;BCP20780;s8592;DB14769;A17073;D11426
Cas No.	1446261-44-4
分子式	C₁₆H₁₅FN₄O
分子量	298.31
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Pamiparib (BGB-290) 是一种有效的，具有口服活性的高选择性 PARP 抑制剂，对 PARP1 和 PARP2 的 IC₅₀ 值分别为 0.9 nM 和 0.5 nM。Pamiparib 能透过血脑屏障，可用于包括实体瘤在内的多种肿瘤的研究。

生物活性

Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC 50 values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor.

性状

Solid

IC50 & Target[1][2]

PARP

体外研究(In Vitro)

Pamiparib shows potent DNA-trapping activity with an IC50 of 13 nM. In the cellular assays, Pamiparib inhibits intracellular PAR formation with an IC50 of 0.24 nM. Tumor cell lines with homologous recombination defects are profoundly sensitive to Pamiparib. Pamiparib is highly active both in vitro and in vivo in BRCA mutant tumors. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Pamiparib suppresses PARP activity in patient-derived glioblastoma multiforme and small-cell-lung cancer xenografts, and potentiates the effects of Temozolamide. In vivo activities of Pamiparib, and its combination activity with chemotherapies in patient biopsy derived small cell lung cancer (SCLC) xenograft models. has not independently confirmed the accuracy of these methods. They are for reference only.

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

ClinicalTrial

参考文献

[1]. Changyou Zhou, et al. Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors. WO 2013097225 A1.
[2]. Friedlander M, et al. Pamiparib in combination with tislelizumab in patients with advanced solid tumours: results from the dose-escalation stage of a multicentre, open-label, phase 1a/b trial. Lancet Oncol. 2019 Sep;20(9):1306-1315.

溶解度数据	In Vitro: DMSO : 50 mg/mL (167.61 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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