化合物CX5461 T2100
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
1 mg | 1138549-36-6 | ¥258.00 | 询底价 |
50 mg | 1138549-36-6 | ¥3,320.00 | 询底价 |
100 mg | 1138549-36-6 | ¥4,750.00 | 询底价 |
500 mg | 1138549-36-6 | ¥9,820.00 | 询底价 |
10 mg | 1138549-36-6 | ¥1,490.00 | 询底价 |
5 mg | 1138549-36-6 | ¥913.00 | 询底价 |
25 mg | 1138549-36-6 | ¥2,350.00 | 询底价 |
2 mg | 1138549-36-6 | ¥412.00 | 询底价 |
Product Introduction
Bioactivity
英文名: CX-5461
描述: CX5461 是一种口服有效的rRNA 合成抑制剂,可抑制 Pol I 驱动的 rRNA 转录。
细胞实验: Cells are plated on 96-well plates and treated the next day with dose response of CX-5461 for 96 hours. Cell viability is determined using Alamar Blue and CyQUANT assays(Only for Reference)
激酶实验: Pol I and Pol II Transcription Assay: Two short-lived RNA transcripts (half-lives ~20-30 minutes), one produced by Pol I and another by Pol II, are quantitated by qRT-PCR as a measure of CX-5461-related effects on transcription. The 45S pre-rRNA served as the Pol I transcript and the mRNA for the protooncogene c-myc served as the comparator Pol II transcript. Both Pol I and Pol II transcription are known to be affected by general cellular stress. To minimize the potential effects of such stress, cells are exposed to test agents for only a short period of time (2 hours). This is sufficient time for these transcripts to be reduced by greater than 90% if CX-5461 affects their synthesis.
体外活性: 在HCT-116(EC50=167 nM),A375(EC50=58 nM),和MIA PaCa-2(和EC50=74 nM)细胞系中,CX-5461能够抑制细胞增殖。在固体肿瘤细胞中,CX-5461诱导细胞自噬或衰老,但不诱导细胞凋亡,其中qi黑色素瘤 A375 (Pol I IC50 = 113 nM;Pol II IC50 > 25 μM)和胰腺癌MIA PaCa-2 (Pol I IC50=54 nM;Pol II IC50 ~25 mM)。在HCT-116细胞中,CX-5461选择性抑制rRNA合成,Pol I(IC50=142 nM),Pol II (IC50 > 25 μM)。
体内活性: 在异种移植人固体肿瘤的小鼠模型中,通过口服CX-5461(50 mg/kg)表现出抗实体瘤活性.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : < 1 mg/mL
H2O : 5.1 mg/mL (10 mM)
关键字: Inhibitor | CX 5461 | CX5461 | CX-5461 | DNA/RNA Synthesis | inhibit
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相关库: Drug Repurposing Compound Library | Anti-Breast Cancer Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Clinical Compound Library | Highly Selective Inhibitor Library | Anti-Cancer Active Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途