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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-AZD9574
AZD9574

Chemical Structure : AZD9574

CAS No.: 2756333-39-6

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AZD9574 (AZD-9574, AZD 9574)

货号: PC-72899Not For Human Use, Lab Use Only.

AZD9574 (AZD-9574) is a potent, selective and CNS penetrant PARP1 inhibitor, inhibits PARP1 enzymatic activity with IC50 of 0.3-2.0 nM in a panel of cell lines irrespective of the HRR status.

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5 mg ￥2280 In stock
10 mg ￥3580 In stock
25 mg ￥5480 In stock
50 mg ￥8580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: 98.58% Select Batch:

生物&药学活性

AZD9574 (AZD-9574) is a potent, selective and CNS penetrant PARP1 inhibitor, inhibits PARP1 enzymatic activity with IC50 of 0.3-2.0 nM in a panel of cell lines irrespective of the HRR status.
AZD9574 acts by selectively inhibiting and trapping PARP1 at the sites of SSBs.
AZD9574 exhibits >8000-fold selectivity for PARP1 compared to PARP2 and other members of the PARP family (PARP2, PARP3, PARP5a and PARP6) in biochemical assays.
AZD9574 inhibits colony formation assay in isogenic cell lines pairs confirmed higher potency and selectivity towards HRD+ models (DLD1 BRCA2-/-; SKOV-3 BRCA2-/- and SKOV-3 PALB2-/-), inhibits BRCA2-/- DLD1 cells with IC50 of 1.38 nM, and shows no effect against BRCA2wt cells.
AZD9574 demonstrated dose-dependent efficacy in a BRCA1 mutant MDA-MB-436 subcutaneous xenograft model. AZD9574 (3 mg/kg) showed sustained tumour growth suppression resulting in a significantly extended survival of tumour-bearing intracranial xenograft model of breast cancer brain metastases.

物理化学性质&存储条件

分子量 428.44
分子式 C21H22F2N6O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

6-fluoro-5-(4-((5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl)piperazin-1-yl)-N-methylpicolinamide

参考文献

1. Kunzah Jamal, et al. Cancer Res (2022) 82 (12_Supplement): 2609.

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