AZD-9574|2756333-39-6|-陌孚医药/Medlife

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AZD-9574

目录号: PL10049 纯度: ≥99%

CAS No. :2756333-39-6

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中文名称	AZD-9574
英文名称	AZD-9574
英文别名	2-Pyridinecarboxamide, 6-fluoro-5-[4-[(5-fluoro-3,4-dihydro-2-methyl-3-oxo-6-quinoxalinyl)methyl]-1-piperazinyl]-N-methyl-;AZD-9574;AZD9574
Cas No.	2756333-39-6
分子式	C₂₁H₂₂F₂N₆O₂
分子量	428.44
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

AZD-9574 是一种有效的，具有血脑屏障的通透性 PARP1 抑制剂，与 PARP2/3/5a/6 相比，对 PARP1 表现出 >8000 倍的选择性。AZD-9574 在 SSB 位点选择性抑制 PARP1。AZD-9574 是一种抗癌化合物，可用于 HRD⁺ 乳腺癌和晚期实体恶性肿瘤研究。

生物活性

AZD-9574 is a potent and brain penetrant PARP1 inhibitor and shows >8000-fold selectivity for PARP1 compared to PARP2/3/5a/6. AZD-9574 acts by selectively inhibiting and trapping PARP1 at the sites of SSBs. AZD-9574 is an anti-cancer agent and can be used for HRD breast cancer and advanced solid malignancies research.

性状

Solid

IC50 & Target[1][2]

PPAR

体外研究(In Vitro)

AZD-9574 inhibits PARP1 enzymatic activity with IC50s range between 0.3-2 nM in all tested cell lines irrespective of the homologous recombination repair (HRR) status.
In isogenic cell lines pairs confirms higher potency and selectivity towards HRR-deficient (HRD) models (DLD1 BRCA2; SKOV-3 BRCA2 and SKOV-3 PALB2). The IC50 in BRCA2 DLD1 cells is 1.38 nM compared to IC50 >40 μM BRCA2 cells. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

AZD-9574 (3 mg/kg) shows sustained tumour growth suppression resulting in a significantly extended survival of tumour-bearing mice, in intracranial xenograft model of breast cancer brain metastases. 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]. Hybrid meeting divulges structures of drug candidates
[2]. 1.Kunzah Jamal, et al. Abstract 2609: AZD9574 is a novel, brain penetrant PARP-1 selective inhibitor with activity in an orthotopic, intracranial xenograft model with aberrant DNA repair. Cancer Res (2022) 82 (12_Supplement): 2609.

溶解度数据	In Vitro: DMSO : 22.22 mg/mL (51.86 mM; ultrasonic and adjust pH to 4 with HCl)DMSO : 8.33 mg/mL (19.44 mM; ultrasonic and warming and heat to 60°C)

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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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