CX-5461 [1138549-36-6]
Référence T2100-5mg
Conditionnement : 5mg
Marque : TargetMol
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CX-5461
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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.
Cas No. 1138549-36-6
With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.4%
Color:White
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Chemical Properties
Storage & Solubility Information
| Description | 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. |
| Targets & IC50 | Pol I-driven transcription of rRNA:142 nM |
| In vitro | Method: 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. Result: Carviolin showed antifungal activity with MIC less than 200 µg/mL against all three fungi. [1] |
| In vivo | In a mouse model of xenograft human solid tumors, oral administration of CX-5461 (50 mg/kg) demonstrated antitumor activity against solid tumors. |
| Kinase Assay | 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. |
| Cell Research | 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) |
| Molecular Weight | 513.614 |
| Formula | C27H27N7O2S |
| Cas No. | 1138549-36-6 |
| Smiles | CN1CCCN(CC1)C1=CC=C2C(=O)C(C(=O)NCC3=CN=C(C)C=N3)=C3SC4=C(C=CC=C4)N3C2=N1 |
| Relative Density. | 1.45 g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | 0.1 M HCl: 25.00 mg/mL (48.67 mM), Sonictaion and heating are recommended.  DMSO: 1.00 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. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/H2O/0.1 M HCl
H2O/0.1 M HCl
0.1 M HCl
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||