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Niraparib hydrochloride (MK-4827 hydrochloride) 是一种具有口服活性的PARP1和PARP2抑制剂,IC50值分别为 3.8 nM 和 2.1 nM。它抑制 DNA 损伤修复,诱导凋亡并具有抗肿瘤活性。

Niraparib hydrochloride (MK-4827 hydrochloride) 是一种具有口服活性的PARP1和PARP2抑制剂,IC50值分别为 3.8 nM 和 2.1 nM。它抑制 DNA 损伤修复,诱导凋亡并具有抗肿瘤活性。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 2 mg | ¥ 297 | In stock | |
| 5 mg | ¥ 462 | In stock | |
| 10 mg | ¥ 797 | In stock | |
| 25 mg | ¥ 1,770 | In stock | |
| 50 mg | ¥ 3,210 | In stock | |
| 100 mg | ¥ 4,630 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 548 | In stock |
Niraparib hydrochloride 相关产品
| 产品描述 | Niraparib hydrochloride (MK-4827 hydrochloride) is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. Niraparib hydrochloride inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single-strand DNA breaks by the base-excision repair (BER) pathway. |
| 靶点活性 | PARP1:3.8nM, tankyrase 1:570 nM, PARP4:330 nM, PARP3:1300 nM, PARP2:2.1 nM |
| 体外活性 | MK-4827可使辐射对人类肿瘤移植体(p53野生型或p53突变型)的效果明显增强.其在体内具有良好耐受性.单独使用时,对BRCA-1缺陷型移植瘤模型也有一定功效. |
| 体内活性 | 在细胞试验中,MK-4827对PARP的活性有抑制效果(EC50:4 nM),并使携带BRCA-1/2突变的癌细胞增殖受抑制(IC50:10-100 nM)。它能有效地抑制PARP-1/2(IC50:3.8/2.1 nM),对PARP-3,V-PARP和tankyrase-1的选择性低100倍以上(IC50:1300/330/570 nM)。在携带BRCA-1突变的MDA-MB-436人类乳腺腺癌的细胞中,MK-4827的CC50为18 nM;在BRCA-2缺陷的CAPAN-1人胰腺癌细胞中,CC50为90 nM。而正常人类前列腺和乳腺上皮细胞对MK-4827具有耐药性。这表明PARP抑制剂在具有BRCA-1/2突变的癌细胞中具有选择性细胞毒性,对周围组织影响小。 |
| 别名 | 尼拉帕利盐酸盐, MK-4827 hydrochloride, MK-4827 (hydrochloride) |
| 分子量 | 356.85 |
| 分子式 | C19H21ClN4O |
| CAS No. | 1038915-64-8 |
| Smiles | C(N)(=O)C=1C=2C(=CN(N2)C3=CC=C(C=C3)[C@@H]4CCCNC4)C=CC1.Cl |
| 密度 | 1.343 g/cm3 |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | H2O: 180 mg/mL (504.41 mM), Sonication is recommended. DMSO: 50 mg/mL (140.11 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.6 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO/H2O
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