CX-5461 is a potent small-molecule rRNA synthesis inhibitor with an IC50 of 0.11 μM. CX-5461 selectively blocks RNA PolI transcription,PIC assembly and SL1-rDNA interaction. CX-5461 indicates potent antiproliferative activity in cancer cells and induces autophagy incancer cells. CX-5461 shows potent antitumor activity in A375 and MiaPaca xenografts.
|Source||J Exp Clin Cancer Res (2018). Figure 4. CX-5461|
|Cell Lines||GBM cells|
|Incubation Time||48 h|
|Results||CX-5461 could lead to a significant decrease of hTERT-FL in a dose-dependent manner and had no effect on hTERT-All|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
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