Taladegib (LY2940680) 1258861-20-9

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Molecular Weight: 512.5 Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.

Biological Activity

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 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.

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Product Categories : Stem Cells & Wnt > Hedgehog/Smoothened Inhibitor