LY2603618 (IC-83) is a highly selective Chk 1 inhibitor with potential antitumor activity. LY2603618 (IC-83) binds to and inhibits the activity of chk1, which may prevent the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents.
|Source||Oncotarget (2017). Figure 2. LY2603618|
|Cell Lines||U2OS cells|
|Concentrations||0, 25, 50 or 100 nM|
|Incubation Time||24 hours|
|Results||An exposure time of 24 hours to the inhibitors was chosen for the clonogenic survival assays to resemble a transient delivery of such inhibitors upon in vivo single injections.|
|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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CCT241533 hydrochloride is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM.
CCT241533 is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM.
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