Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM. Cyclopamine blocks the oncogenic effects of mutations of Ptch in fibroblasts and inhibits the growth of cells lacking Ptch function. Cyclopamine induced apoptosis in several small-cell lung cancer cell lines at 5 µM. Cyclopamine also be used to induce differentiation of human embryonic stem cells (hESCs) into hormone-expressing endocrine cells. Cyclopamine (11-deoxojervine) depletes stem-like cancer cells in glioblastoma and blocks tumor engraftment. Cyclopamine treatment significantly decreases of Snail mRNA and increasea E-cadherin transcripts in the E3LZ10.7 cell line in vitro. Administration of Cyclopamine alone profoundly inhibits tumor metastases in xenografts of E3LZ10.7 and L3.6pl, and completely abrogates metastases when in combination of gemcitabine.
|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 5 mg/mL|
Synthesis and anticancer activity studies of cyclopamine derivatives.
Zhang J, et al. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1359-63. PMID: 18221872.
Cyclopamine-mediated hedgehog pathway inhibition depletes stem-like cancer cells in glioblastoma.
Bar EE, et al. Stem Cells. 2007 Oct;25(10):2524-33. PMID: 17628016.
Effects of oncogenic mutations in Smoothened and Patched can be reversed by cyclopamine.
Taipale J, et al. Nature. 2000 Aug 31;406(6799):1005-9. PMID: 10984056.
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