1258861-20-9
中文名称
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
英文名称
LY2940680
CAS
1258861-20-9
分子式
C26H24F4N6O
分子量
512.51
MOL 文件
1258861-20-9.mol
更新日期
2024/07/16 10:37:41
1258861-20-9 结构式
基本信息
中文别名
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
LY2940680Taladegib
LY2940680 USP/EP/BP
LY2940680 (Taladegib)
LY 2940680
LY2940680
Taladegib (LY2940680)
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-(2-Methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-2-(trifluoroMethyl)benzaMide
4-fluoro-N-Methyl-N-(1-(4-(1-Methyl-1H-pyrazol-5-yl)phthalazin-1-yl)piperidin-4-yl)-2-(trifluoroMethyl)benzaMide
所属类别
生物化工：Hedgehog/Smoothened 抑制剂物理化学性质
沸点703.5±60.0 °C(Predicted)
密度1.39
储存条件-20°C储存
溶解度insoluble in H2O; ≥5.2 mg/mL in EtOH with ultrasonic; ≥51.3 mg/mL in DMSO with gentle warming and ultrasonic
酸度系数(pKa)7.94±0.30(Predicted)
形态结晶固体
颜色White to off-white
常见问题列表
生物活性
Taladegib (LY2940680)与Smoothened(Smo)受体结合，有效抑制Hedgehog(Hh)信号通路。Phase 1/2。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.靶点
| Target | Value |
| Smoothened |