| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| S409208-1ml |
1ml |
现货  |
|
| 英文别名 | Erismodegib | [1,1'-Biphenyl]-3-carboxamide, N-[6-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-3-pyridinyl]-2-methyl-4'-(trifluoromethoxy)-, rel- |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Sonidegib (NVP-LDE225) |
| 生化机理 | Sonidegib（Erismodegib，NVP-LDE225）是一种Smoothened（Smo）拮抗剂，可抑制Hedgehog（Hh）信号传导，在无细胞实验中的IC50分别为1.3 nM（小鼠）和2.5 nM（人类）。第 3 阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 拮抗剂 |
| 作用机制 | SMO 的拮抗剂 |
| 产品介绍 |
LDE225 (NVP-LDE225,Erismodegib)是一种Smoothened(Smo)拮抗剂，抑制Hedgehog (Hh)信号通路，IC50分别为1.3 nM (小鼠)和2.5 nM(人)。 Information Sonidegib (Erismodegib, NVP-LDE225) is aSmoothened(Smo) antagonist, inhibitingHedgehog(Hh) signaling withIC50of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3. Sonidegib (Erismodegib, NVP-LDE225) inhibits TM3 luciferized cell line with 0.6 nM and 8 nM, at the presence of 1 nM and 25 nM Hh agonist Ag1.5, respectively. In vivo Sonidegib (Erismodegib, NVP-LDE225) is highly bound to mouse, rat, and human plasma proteins (>99%) and moderately bound to dog and monkey plasma proteins (77 and 85%, respectively). LDE225 has high permeability (90.8% in man) in the PAMPA assay. LDE225 shows good oral bioavailability ranging from 69 to 102% in preclinical species when dosed in solution. LDE225 is a weak base with a measured pKa of 4.20 and exhibits relatively poor aqueous solubility. LDE225 demonstrates dose-related antitumor activity. At a dose of 5 mg/kg/day qd, LDE225 significantly inhibits tumor growth, corresponding to a T/C value of 33%. When dosed at 10 and 20 mg/kg/day qd, LDE225 gives rise to 51 and 83% regression, respectively. Gli1 mRNA inhibition correlates with tumor and plasma exposure of LDE225. LDE225 successfully penetrates the blood−brain barrier in tumor-bearing animals and results in tumor growth inhibition after 4 days of treatment. LDE225 significantly reduces the tumor volume by 95.7% in Rip1-Tag2 mice. LDE225 prolongs survival in Rip1Tag2 mice. LDE225 decreases expression of stromal markers in the LDE225-treated mice. cell lines： Concentrations：~10 μM Incubation Time：30 minutes Powder Purity:≥99% |
| IC50 | Smo (mouse), IC50: 1.3 nM; Smo (human), IC50: 2.5 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CC1CN(CC(C)O1)C2=CC=C(NC(=O)C3=C(C)C(=CC=C3)C4=CC=C(OC(F)(F)F)C=C4)C=N2 |
| 分子量 | 485.5 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 57 mg/mL (198.37 mM); Ethanol: 2 mg/mL (6.96 mM); Water: Insoluble; |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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