规格

价格

库存

数量

1 mg

¥ 258

现货

2 mg

¥ 412

现货

5 mg

¥ 913

现货

10 mg

¥ 1,490

现货

25 mg

¥ 2,350

现货

50 mg

¥ 3,320

现货

100 mg

¥ 4,750

现货

500 mg

¥ 9,820

现货

生物活性

产品描述	CX5461 is an rRNA synthesis inhibitor with oral activity that inhibits Pol I-driven rRNA transcription. CX5461 activates the DNA damage response and has antitumor activity in tumors such as ovarian cancer.
靶点活性	Pol I-driven transcription of rRNA:142 nM
体外活性	方法：HCT-116、A375、MIA PaCa-2 和 BJ hTERT 细胞用 CX5461 (0-10 µM) 处理 96 h，通过 CyQUANT assay 检测细胞活力。结果：HCT-116、A375 和 MIA PaCa-2 细胞系的抗增殖剂量反应评估分别得出了 167、58 和 74 nmol/L 的 EC50。BJ-hERT 正常细胞系的 EC50 约为 5000 nmol/L。[1] 方法：CaSki 细胞用 CX5461 (1-5 µM) 处理 24-72 h，通过 Western Blot 检测靶点蛋白表达水平。结果：CX5461 处理后，LC3I 完全转化为 LC3II，同时 p62 表达减少。LC3I 和 LC3II 条带的密度测定分析显示，CX5461 治疗 72 h 后，LC3II:LC3I 比值显著增加。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 CX5461 (50 mg/kg，50 mmol/L NaH2PO4 pH 4.5) 口服给药给携带 MIA PaCa-2 或 A375 异种移植物的小鼠，每天一次或每三天一次，持续 32 天。结果：CX5461 在第 31 天显示出明显的 MIA PaCa-2 TGI，TGI 等于 69%。同样，CX5461 显示出明显的 A375 TGI，第 32 天的 TGI 等于 79%。[1]
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.
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)

化学信息

分子量	513.61
分子式	C₂₇H₂₇N₇O₂S
CAS No.	1138549-36-6
Smiles	CN1CCCN(CC1)c1ccc2c(n1)n1c3ccccc3sc1c(C(=O)NCc1cnc(C)cn1)c2=O
密度	1.45 g/cm3

储存&溶解度

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

DMSO: 1 mg/mL (1.95 mM), Sonication is recommended.

H2O: 5.15 mg/mL (10.03 mM), when pH is adjusted to 7 with HCl. Sonication is recommended.

溶液配制表

DMSO/H2O

	1mg	5mg	10mg	50mg
1 mM	1.9470 mL	9.7350 mL	19.4700 mL	97.3501 mL

H2O

	1mg	5mg	10mg	50mg
5 mM	0.3894 mL	1.9470 mL	3.8940 mL	19.4700 mL
10 mM	0.1947 mL	0.9735 mL	1.9470 mL	9.7350 mL

CX-5461

CX-5461

产品介绍

计算器

体内实验配液计算器

剂量转换

引用文献

关键词

CX-5461

CX-5461

CX-5461 相关产品

产品介绍

计算器

体内实验配液计算器

剂量转换

引用文献

关键词