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- 2025年12月05日
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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1262417-51-5
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥826.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥429.0 |
| 规格： | 5 mg | 产品价格： | ￥950.0 |
| 规格： | 10 mg | 产品价格： | ￥1520.0 |
| 规格： | 25 mg | 产品价格： | ￥3040.0 |
| 规格： | 50 mg | 产品价格： | ￥4600.0 |
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NMS-P118
CAS No. : 1262417-51-5
MCE 国际站：NMS-P118
产品活性：NMS-P118是一种有效的，口服可用的，高选择性的PARP-1抑制剂，在HeLa细胞中的IC50值为0.04 μM。
研究领域：Cell Cycle/DNA Damage | Epigenetics
作用靶点：PARP
In Vitro: NMS-P118 is found to be less myelotoxic in vitro than olaparib, a dual PARP-1/-2 inhibitor. NMS-P118 proves to be metabolically stable, it modestly inhibits two cytochrome P450 family members (CYP-2B6 IC50: 8.15 μM; CYP-2D6 IC50: 9.51 μM) out of eight isoforms tested. Its ability in hampering the proliferation of bone marrow cells is from 5 to > 60 times lower then olaparib according to the species.
In Vivo: NMS-P118 is a potent (KD=0.009 μM) PARP-1 inhibitor, showing 150-fold selectivity over PARP-2 (KD=1.39 μM). NMS-P118 possesses excellent pharmacokinetic profile and nearly complete oral bioavailability both in mice and rats. It proved to be highly efficacious in vivo both as single agent in MDA-MB-436 human breast cancer tumors and in combination with temozolomide in CAPAN-1 human pancreatic tumors growing as xenografts in the mouse. The compound is well tolerated at highly efficacious doses and is endowed with an excellent ADME profile.
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文献和实验Practical Aspects of Radioligand Binding
Figure 1.3.1 Saturation binding to muscarinic receptors on N1E‐115 mouse neuroblastoma cells. Six concentrations of [3 H] N ‐methylscopolamine ([3 H]NMS), with or without 10 µM unlabeled NMS, were incubated
-0669 镊子头P-610P-1 镊子头P-610P-1 HOZAN-70045 精密镊子P-840 P-840 HOZAN-0668 镊子P-610-P 镊子P-610-P HOZAN-0181 切割刀片K-110-2 切割刀片K-110-2 HOZAN-0018 斜口钳N-5-150 斜口钳N-5-150 HOZAN-0028 尖嘴钳P-15-150 尖嘴钳P-15-150 HOZAN-0062 镊子P-898 镊子P-898 HOZAN-0016 斜口钳N-9-150
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