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
生物活性体外研究体内研究生物活性靶点 用途与合成方法 MSDS 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)苯甲酰胺价格(试剂级) 上下游产品信息
| 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 |
|---|---|
| 中文同义词 | 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);化合物TALADEGIB;LY2940680,刺猬信号通路抑制剂 |
| 英文名称 | LY2940680 |
| 英文同义词 | Taladegib (LY2940680);4-Fluoro-N-methyl-N-[1-[4-(1-methyl-1H-pyrazol-5-yl)-1-phthalazinyl]-4-piperidinyl]-2-(trifluoromethyl)benzamide LY 2940680;LY2940680;LY2940680 (Taladegib);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 |
| CAS号 | 1258861-20-9 |
| 分子式 | C26H24F4N6O |
| 分子量 | 512.5 |
| EINECS号 | |
| 相关类别 | 信号转导通路激酶抑制剂;干细胞与Wnt信号;小分子抑制剂,天然产物;小分子抑制剂;抑制剂;活性分子;Inhibitors |
| Mol文件 | 1258861-20-9.mol |
| 结构式 | ![]() |
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 性质
| 沸点 | 703.5±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.39 |
| 储存条件 | Store at -20°C |
| 溶解度 | 不溶于水; ≥5.2 mg/mL,乙醇溶液,超声波; DMSO 中≥51.3 mg/mL,温和加热和超声波 |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 7.94±0.30(Predicted) |
| 颜色 | 白色至米白色 |
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 用途与合成方法
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.
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。
靶点
| Target | Value |
| Smoothened |
安全信息
MSDS信息
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 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-13242 | Taladegib | 1 mg | 500元 | |
| 2024/08/19 | HY-13242 | 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 Taladegib | 1258861-20-9 | 5mg | 1100元 |



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