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LDE225 (NVP-LDE225,Erismodegib) Sale

(Synonyms: 索尼吉布,Erismodegib; LDE225; NVP-LDE225) 目录号 : GC13655

LDE225 (NVP-LDE225,Erismodegib) (Erismodegib) 是一种有效的选择性 Smo 拮抗剂,在结合试验中对小鼠和人 Smo 的 IC50 分别为 1.3 nM 和 2.5 nM。

LDE225 (NVP-LDE225,Erismodegib) Chemical Structure

Cas No.:956697-53-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥410.00
现货
5mg
¥389.00
现货
10mg
¥546.00
现货
50mg
¥1,166.00
现货
100mg
¥1,754.00
现货
200mg
¥3,308.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

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.

产品描述

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.

Chemical Properties

Cas No. 956697-53-3 SDF
别名 索尼吉布,Erismodegib; LDE225; NVP-LDE225
化学名 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
分子式 C26H26F3N3O3 分子量 485.5
溶解度 ≥ 24.3mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.0597 mL 10.2987 mL 20.5973 mL
5 mM 0.4119 mL 2.0597 mL 4.1195 mL
10 mM 0.206 mL 1.0299 mL 2.0597 mL
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