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AZD-2461
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AZD-2461
CAS No. : 1174043-16-3
MCE 站:AZD-2461
产品活性:AZD-2461 是一种有效的 PARP 抑制剂,可抑制 PARP1,PARP2 和 PARP3 的活性,IC50 值分别为 5 nM,2 nM 和 200 nM。
研究领域:Cell Cycle/DNA Damage | Epigenetics
作用靶点:PARP
In Vitro: AZD-2461 is a potent PARP inhibitor, with IC50s of 5 nM, 2 nM and 200 nM for PARP1, PARP2 and PARP3, respectively. AZD-2461 (500 nM) shows inhibitory activity against DNA single-strand break repair in human A459 cells. AZD-2461 cuases resistance and high P-gp expression levels in BRCA2-deficient mouse breast cancer line KB2P3.4. AZD-2461 is cytotoxic to BT-20 cells (5-50 μM), increases the proportions of S- and G2-phase BT-20 cells (5-20 μM), and weakly affects the progression of cell cycle in SKBr-3 cells (5-20 μM).
In Vivo: AZD-2461 (10 mg/kg, p.o.) enhances the antitumor activity of temozolomide in a mouse colorectal xenograft and exhibits low effect on mouse bone marrow cells. However, the increased bone marrow tolerability of AZD-2461 is not seen in rat models. AZD-2461 (0.5% v/w HPMC, p.o.) increases the survival of mice bearing KB1P tumors after short-term treatment, and long-term treatment is well tolerated, but can not lead to tumor eradication.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | XAV-939 | Rucaparib | PJ34 | 3-Aminobenzamide | G007-LK | Dehydrocorydaline chloride | AG14361 | Iniparib | BGP-15 | Fucosterol | JW 55 | EB-47 dihydrochloride | UPF 1069 | AZ6102 | iRucaparib-AP6 | ME0328 | MN-64 | 5,?7,?4'-?Trimethoxyflavone | Benzamide | GeA-69 | Paris saponin VII | PARP14 inhibitor H10 | BYK204165 | NU1025 | Oroxin A | 2-Methylquinazolin-4-ol
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