| Molecular Formula | C26H24F4N6O |
| Molar Mass | 512.5 |
| Density | 1.39 |
| Boling Point | 703.5±60.0 °C(Predicted) |
| Solubility | DMSO 0.66 mg/mL (1.28 mM); Water <1 mg/mL (<1 mM); Ethanol 2 mg/mL (3.9 mM) |
| pKa | 7.94±0.30(Predicted) |
| Storage Condition | -20℃ |
| MDL | MFCD21609264 |
| In vitro study | 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 study | 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. |
| biological activity | Taladegib (LY2940680) binds to Smoothened(Smo) receptor to effectively inhibit Hedgehog(Hh) signaling pathway. Phase 1/2. Taladegib (LY2940680) binds to Smoothened(Smo) receptor to effectively inhibit Hedgehog(Hh) signaling pathway. Phase 1/2. |
| in vitro study | 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 study | LY2940680 has excellent pharmacokinetic properties in rodent and non-rodent species. LY2940680 administrated orally treat 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. |
| target | TargetValue Smoothened |
| Target | Value |