Rabusertib (LY2603618) is an effective and selective Chk1 inhibitor with an IC50 of 7 nM.
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Solubility||DMSO 12 mg/mL|
|Related Checkpoint Products|
WAY-239320 is a Chk1 inhibitor
Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM.
Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM.
GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.
CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.
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