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PARP1-IN-5 dihydrochloride 是一种具有口服活性的有效选择性 PARP-1 抑制剂 (IC50 =14.7 nM)。它可用于癌症的研究。
PARP1-IN-5 dihydrochloride 是一种具有口服活性的有效选择性 PARP-1 抑制剂 (IC50 =14.7 nM)。它可用于癌症的研究。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 860 | 现货 | |
5 mg | ¥ 1,950 | 现货 | |
10 mg | ¥ 3,150 | 现货 | |
25 mg | ¥ 4,970 | 现货 | |
50 mg | ¥ 6,990 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 2,580 | 现货 |
产品描述 | PARP1-IN-5 dihydrochloride is an orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer. |
靶点活性 | PARP2:0.9 μM, PARP1:14.7 nM |
体外活性 | PARP1-IN-5 dihydrochloride 在0.1~10μM浓度范围内能显著增强CBP对A549细胞的细胞毒性,表现出剂量依赖性。同时,PARP1-IN-5 dihydrochloride 能降低SK-OV-3细胞中MCM2-7的表达。在0.1~320μM的浓度下,PARP1-IN-5 dihydrochloride 对A549细胞的细胞毒性效应较弱。它能显著降低SK-OV-3细胞上的PAR水平。PARP1-IN-5 dihydrochloride 通过PARP-1发挥抗肿瘤作用,并能增加γ-H2AX的表达。 |
体内活性 | PARP1-IN-5 dihydrochloride (1000 mg/kg;口服)显示体重和血常规[1]没有显著差异。PARP1-IN-5 dihydrochloride (25和50 mg/kg;口服;12天)在50 mg/kg时显著增强了卡铂对A549细胞的抑制效果[1]。PARP1-IN-5 dihydrochloride (50 mg/kg;口服)与PARP-1表达量正相关[1]。PARP1-IN-5 dihydrochloride 能降低PAR表达,并上调γ-H2AX表达[1]。 |
分子量 | 537.46 |
分子式 | C25H26Cl2N2O5S |
CAS No. | 2823308-89-8 |
Smiles | O=C1C=C(C2=CC=C(O)C=C2)OC3=C(CN4CCN(CC5=CC=CS5)CC4)C(O)=CC(O)=C31.Cl[H].Cl[H] |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 125 mg/mL (232.58 mM), Sonication is recommended. H2O: 1 mg/mL (1.86 mM), Sonication and heating to 60℃ are recommended. | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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