中文名 | 4-氟-N-甲基-N-[1-[4-(1-甲基-1H-吡唑-5-基)-1-酞嗪基]-4-哌啶基]-2-(三氟甲基)苯甲酰胺 |
英文名 | LY2940680 |
别名 | 化合物TALADEGIB 4-氟-N-甲基-N-[1-[4-(1-甲基-1H-吡唑-5-基)-1-酞嗪基]-4-哌啶基]-2-(三氟甲基)苯甲酰胺 4-氟-N-甲基-N-[1-[4-(1-甲基-1H-吡唑-5-基)-1-酞嗪基]-4-哌啶基]-2-(三氟甲基)苯甲酰胺(LY2940680) |
英文别名 | LY2940680 Taladegib Taladegib (LY2940680) LY2940680 (Taladegib) Taladegib hydrochloride 4-Fluoro-N-methyl-N-(1-(4-(1-methyl-1H-pyrazol-5-yl)phthalazin-1-yl)piperidin-4-yl)-2-(trifluo 4-Fluoro-N-methyl-N-[1-[4-(1-methyl-1H-pyrazol-5-yl)-1-phthalazinyl]-4-piperidinyl]-2-(trifluoromethyl)benzamide 4-Fluoro-N-methyl-N-[1-[4-(1-methyl-1H-pyrazol-5-yl)-1-phthalazinyl]-4-piperidinyl]-2-(trifluoromethyl)benzamide LY 2940680 |
CAS | 1258861-20-9 |
化学式 | C26H24F4N6O |
分子量 | 512.5 |
密度 | 1.39 |
沸点 | 703.5±60.0 °C(Predicted) |
溶解度 | DMSO 0.66 mg/mL (1.28 mM); 水 <1 mg/mL (<1毫米); 乙醇2 mg/mL (3.9 mM) |
酸度系数 | 7.94±0.30(Predicted) |
存储条件 | -20℃ |
MDL号 | MFCD21609264 |
体外研究 | 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. |
体内研究 | 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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