4-Fluoro-N-methyl-N-[1-[4-(1-methyl-1H-pyrazol-5-yl)-1-phthalazinyl]-4-piperidinyl]-2-(trifluoromethyl)benzamide LY 2940680 - Names and Identifiers
4-Fluoro-N-methyl-N-[1-[4-(1-methyl-1H-pyrazol-5-yl)-1-phthalazinyl]-4-piperidinyl]-2-(trifluoromethyl)benzamide LY 2940680 - Physico-chemical Properties
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. |
4-Fluoro-N-methyl-N-[1-[4-(1-methyl-1H-pyrazol-5-yl)-1-phthalazinyl]-4-piperidinyl]-2-(trifluoromethyl)benzamide LY 2940680 - Introduction
LY2940680 binds to Smoothened(Smo) receptor and effectively inhibits Hedgehog(Hh) signaling pathway. Phase 1/2.
Last Update:2022-10-16 17:41:23
4-Fluoro-N-methyl-N-[1-[4-(1-methyl-1H-pyrazol-5-yl)-1-phthalazinyl]-4-piperidinyl]-2-(trifluoromethyl)benzamide LY 2940680 - Reference Information
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 |
Last Update:2024-04-09 19:05:03