For research use only.
CAS No. 1258861-20-9
Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.
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Choose Selective Hedgehog/Smoothened Inhibitors
|Description||Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.|
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. 
|In vivo||LY2940680 has excellent pharmacokinetic properties in rodent and non-rodent species. LY2940680 administrated orally treats Ptch+/- p53-/- transgenic mice which spontaneously develop medulloblastoma, produces remarkable efficacy and significantly improves their survival. LY2940680 reveals rapid kinetics of anti-tumor activity through magnetic resonance imaging of these mice, and LY2940680 induces Caspase-3 activity and reduces proliferation by immunohistochemistry analysis of medulloblastoma tumors. LY2940680 inhibits Hh regulated gene expression in the subcutaneous xenograft tumor stroma and produces significant anti-tumor activity. |
|In vitro||DMSO||5 mg/mL warmed (9.75 mM)|
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|% DMSO % % Tween 80 % ddH2O|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01919398||Completed||Drug: LY2940680||Neoplasm Metastasis||Eli Lilly and Company||August 2013||Phase 1|
|NCT01697514||Withdrawn||Drug: LY2940680||Medulloblastoma Childhood|Rhabdomyosarcoma||Eli Lilly and Company||July 2013||Phase 1|
|NCT01746745||Completed||Drug: [^14C]-LY2940680||Healthy Volunteers||Eli Lilly and Company||January 2013||Phase 1|
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