Sonidegib
产品说明书
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同义名 : | Erismodegib; LDE225; NVP-LDE225 |
| CAS号 : | 956697-53-3 | |
| 货号 : | A154891 | |
| 分子式 : | C26H26F3N3O3 | |
| 纯度 : | 99% | |
| 分子量 : | 485.498 | |
| MDL号 : | MFCD16038928 | |
| 存储条件： |
Pure form Sealed in dry, room temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(102.99 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+45% PEG300+water 1 mg/mL clear PO 0.5% CMC-Na 30 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Smoothened (Smo) is a transmembrane protein that serves as a key activator of the hedgehod (Hh) signaling pathway. LDE225 is a potent and selective Smo antagonist with IC50 values of 1.3 and 2.5nM for mouse and human, respectively[6]. It is tightly bound to human, mouse, and rat plasma proteins (99%), but moderately bound to monkey (85%) and dog (77%) plasma proteins. The combination of LDE225 (20μM) and nilotinib (2μM) more efficiently inhibited the outgrowth of BaF3 cells expressing wt-BCRABL and BCR-ABL mutants as compared to cells treated with either agent alone[4]. In the mouse subcutaneous Ptch+/-p53-/- medulloblastoma allograft model, daily oral administration of LDE225 diphosphate salt (5, 10, or 20mg/kg/day) for 13 days significantly inhibited tumor growth with T/C values of 33%, 51%, and 83%, respectively, as compared to vehicle-treated controls. A single oral dose of LDE225 diphosphate salt (5, 10, or 20mg/kg/day) inhibited Gli1mRNA expression in the mouse medulloblastoma model at a dose- and time-dependent manner[5]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
| 769-P | ~5 μM | Growth inhibitory assay | IC50=2-3 μM | 25093491 | |
| 786-O | ~5 μM | Growth inhibitory assay | IC50=2-3 μM | 25093491 | |
| 786-O SuR | ~5 μM | Growth inhibitory assay | IC50=2-3 μM | 25093491 | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.06mL 0.41mL 0.21mL |
10.30mL 2.06mL 1.03mL |
20.60mL 4.12mL 2.06mL |
| 参考文献 |
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