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LDE225 (NVP-LDE225,Erismodegib)Smoothened inhibitor,potent and selective |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.76%
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- NMR (Nuclear Magnetic Resonance)
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Chemical structure
Related Biological Data
Description | LDE225 is a potent and selective antagonist of Smoothened (Smo) with IC50 values of 2.5 nM and 1.3 nM for human Hedgehog and mouseHedgehog, respectively. | |||||
Targets | human Hedgehog | mouseHedgehog | ||||
IC50 | 2.5 nM | 1.3 nM |
Cell experiment: [1] | |
Cell lines | Cancer stem cells (CSCs) |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
Reaction Conditions | 10 μM, 48 hours (for apoptosis induction)10 μM, 7 days (for cell viability inhibition) |
Applications | LDE225 induced apoptosis in a dose-dependent manner. Treatment of prostate CSCs resulted in an increase in the expression of cleaved caspase-3 and PARP. LDE225 inhibited cell viability in primary and secondary spheroids in a dose-dependent manner. |
Animal experiment: [1] | |
Animal models | NOD/SCID IL2Rγnull mice injected with human prostate CSCs |
Dosage form | Intraperitoneal injection, 20mg/kg body weight, three times per week for 4 weeks |
Applications | NVP-LDE-225 had no effect on body weight of mice. Interestingly, NVP-LDE-225 inhibited CSC tumor growth, as demonstrated by the significant reduction in tumor weight. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Nanta R, Kumar D, Meeker D, et al. NVP-LDE-225 (Erismodegib) inhibits epithelial–mesenchymal transition and human prostate cancer stem cell growth in NOD/SCID IL2Rγ null mice by regulating Bmi-1 and microRNA-128. Oncogenesis, 2013, 2(4): e42. |
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Cas No. | 956697-53-3 | SDF | Download SDF |
Synonyms | N/A | ||
Chemical Name | N-[6-[(2S,6R)-2,6-dimethylmorpholin-4-yl]pyridin-3-yl]-2-methyl-3-[4-(trifluoromethoxy)phenyl]benzamide | ||
Canonical SMILES | CC1CN(CC(O1)C)C2=NC=C(C=C2)NC(=O)C3=CC=CC(=C3C)C4=CC=C(C=C4)OC(F)(F)F | ||
Formula | C26H26F3N3O3 | M.Wt | 485.5 |
Solubility | ≥24.3mg/mL in DMSO | Storage | Store at -20°C |
Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
LDE225 is a potent and selective inhibitor of smoothened with IC50 values of 1.3nM in mouse and 2.5nM in human, respectively [1].
LDE225 is screened out from a high-throughput cell-based screen of in-house diversity combinatorial libraries and is developed to be an antagonist of Smo. Smo is an activator of the hedgehog(Hh) signaling pathway and aberrant activation links to tumorigenesis in several cancers. The antitumor efficacy of LDE225 has been evaluated in vivo. In the subcutaneous Ptch+/-p53-/- medulloblastoma allograft mouse model, LDE225 can significantly inhibit tumor growth at a dose of 5mg/kg/day. And in an orthotopic Ptch+/-p53-/- medulloblastoma allograft model, LDE225 is suggested to penetrate the blood-brain barrier in tumor-bearing animals and cause the tumor growth inhibition after 4 days of treatment. Additionally, the preclinical safety assays show that LDE225 has no genotoxicity and has good selectivity [1].
References:[1] Shifeng Pan, Xu Wu, Jiqing Jiang, et al. Discovery of NVP-LDE225, a potent and selective smoothened antagonist. ACS Med. Chem. Lett. 2010, 1: 130–134.
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荧光原位杂交技术(Florescence In-Situ Hybridization简称FISH)是一种利用非放射性的荧光信号对原位杂交样本进行检测的技术。它将荧光信号的高灵敏度、安全性,荧光信号的直观性和原位杂交的高准确性结合起来,通过荧光标记的DNA探针与待测样本的DNA进行原位杂交,在荧光显微镜下对荧光信号进行辨别和计数,从而对染色体或基因异常的细胞、组织样本进行检测和诊断,为各种基因相关疾病的分型、预前和预后提供准确的依据。自20世纪80年代末,Pinkel和Heiles将FISH技术引入染色体检测领域后,FISH技术就在临床诊断及科研工作中得到了广泛的运用,显示出与一些传统技术相比的明显优势。
与传统的免疫组织化学法(IHC)相比,FISH具有良好的稳定性和可重复性。目前免疫组织化学法正广泛应用于肿瘤等多个领域的临床诊断。免疫组化的检测对象是疾病相关的蛋白。由于蛋白的表达和本身的构象受各种因素的影响很大(例如酸、碱和变性剂),检测条件的稳定性对检测结果至关重要。此外,免疫组化检测结果的判断依赖于检测者对显色结果的主观判断,对于一些弱阳性的结果,不同的检测者容易产生分歧。上述的因素都可能影响医生对病情的最终诊断。荧光原位杂交技术检测的对象是细胞中的DNA,致密的双螺旋结构使DNA可以历经千百万年而依然保持良好,其结构稳定,不易被环境条件影响,为荧光原位杂交技术的稳定提供了良好的基础。此外,荧光原位杂交结果的判定借助于对荧光的颜色判断和信号计数,客观地量化了检测地结果。如果借助于相应的FISH操作系统(例如Abbott-Vysis公司的Hybrit杂交仪和VP2000样本预处理系统)和染色体成像系统(例如AI公司的CytoVision)就能实现整个FISH操作的自动化,最大限度的降低操作者和检测者的主观因素,确保结果的准确性。
PCR由于灵敏度高,操作简便快捷是近年来应用比较多的基因诊断技术,但PCR诊断技术的假阴性和假阳性的比例较高,对同一样本也只能作一次分析,不能重复实验结果。随着探针技术的不断发展,FISH目前的灵敏度已经接近或达到PCR的水平,并能很好弥补PCR技术的局限。FISH技术不仅有极低的假阳性、假阴性的比例(以Abbott-Vysis的产前诊断探针为例,29,000例的使用结果证实正确率高达99.9%),还能对同一样本进行多次的FISH操作以及利用不同颜色的荧光探针一次检测多个染色体或基因的异常,大大节省了检测的时间。此外,通过FISH可以对染色体或特定基因的数目异常,特定片断的缺失、易位和重排进行诊断研究。展开