LY2940680 is a Hedgehog inhibitor in clinical trials. LY2940680 binds to the Smo receptor and potently inhibits Hh signaling. LY2940680 inhibits cancer growth in cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib. LY2940680 induces Caspase-3 activity and reduces proliferation by immunohistochemistry analysis of medulloblastoma tumors. LY2940680 is currently being tested in phase I trials for people with a range of solid tumors.
|Source||PLoS One (2015). Figure 3. LY2940680|
|Cell Lines||CCA Cell|
|Incubation Time||72 h|
|Results||In contrast, Vismodegib, a small-molecule antagonist of Smoothened and LY2940680, a small-molecule antagonist of the smoothened receptor, showed a slight inhibitory effect on cell proliferation without differences between mucin-(IC50: Vismodecib = 61.7 ± 1.4 μM, LY2940680 = 49.8 ± 4.5 μM) and mixed-CCA (IC50: Vismodecib = 81.6 ± 14.8 μM, LY2940680 = 61.2 ± 21.1 μM).|
|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.
|Solubility||Ethanol 2 mg/mL|
Investigational Notch and Hedgehog inhibitors--therapies for cardiovascular disease.
Redmond EM, et al. Expert Opin Investig Drugs. 2011 Dec;20(12):1649-64. PMID: 22007748.
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