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CX-5461
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CX-5461图片
CAS NO:1138549-36-6
包装与价格:
包装价格(元)
1 mg电议
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议

产品介绍
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。

产品描述

CX-5461, a selective inhibitor of rRNA synthesis, suppresses Pol I-driven transcription of rRNA.

体外活性

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.

体内活性

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)。

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)

Cas No.

1138549-36-6

分子式

C27H27N7O2S

分子量

513.62

储存和溶解度

DMSO:5.14 mg/ml (10 mM),Need ultrasonic
H2O:Insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years