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.
|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.
|Related Hedgehog Products|
|Smoothened Agonist (SAG) HCl
Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.
LDE225 Diphosphate is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively.
Jervine is a naturally occuring steroidal alkaloid that causes cyclopia by blocking sonic hedgehog signaling.
GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM.
PF-5274857 is a novel Smoothened antagonist, inhibits Hedgehog signaling with IC50 and Ki values of 5.8 nM and 4.6 nM, respectively.
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