| 名称 | CX-5461 |
| 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. |
| 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 | METHODS: The phytopathogenic fungi A. tubingensis, Nigrospora oryzae and Phoma herbarum were treated with Carviolin (1-512 µg/mL) for 18 h and subjected to Antifungal Assay.
RESULTS: Carviolin showed antifungal activity with MIC less than 200 µg/mL against all three fungi. [1] |
| 体内活性 | In a mouse model of xenograft human solid tumors, oral administration of CX-5461 (50 mg/kg) demonstrated antitumor activity against solid tumors. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 1 mg/mL (1.95 mM), Sonication is recommended.
H2O : 5.1 mg/mL (10 mM), when pH is adjusted to 7 with HCl. Sonication is recommended.
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| 关键字 | Inhibitor | CX 5461 | CX5461 | CX-5461 | DNA/RNA Synthesis | inhibit |
| 相关产品 | Rifampicin | 5-Fluorouracil | Ribavirin | Guanidine hydrochloride | 2,4-D | Resveratrol | Trimethoprim | Azelaic acid | Acyclovir | Thymidine | Temozolomide | Folic acid |
| 相关库 | 高选择性抑制剂库 | 经典已知活性库 | 抗乳腺癌化合物库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 抑制剂库 | 抗衰老化合物库 | 已知活性化合物库 | 抗癌药物库 | 抗癌活性化合物库 |
United States
