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LDE225 (NVP-LDE225,Erismodegib)

Smoothened inhibitor,potent and selective CAS# 956697-53-3

LDE225 (NVP-LDE225,Erismodegib)

Catalog No. BCC5066----Order now to get a substantial discount!

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LDE225 (NVP-LDE225,Erismodegib): 5mg $58 In Stock
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Quality Control of LDE225 (NVP-LDE225,Erismodegib)

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Chemical structure

LDE225 (NVP-LDE225,Erismodegib)

3D structure

Chemical Properties of LDE225 (NVP-LDE225,Erismodegib)

Cas No. 956697-53-3 SDF Download SDF
PubChem ID 24775005 Appearance Powder
Formula C26H26F3N3O3 M.Wt 485.5
Type of Compound N/A Storage Desiccate at -20°C
Synonyms NVP-LDE 225; Erismodegib
Solubility DMSO : 50 mg/mL (102.99 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name N-[6-[(2S,6R)-2,6-dimethylmorpholin-4-yl]pyridin-3-yl]-2-methyl-3-[4-(trifluoromethoxy)phenyl]benzamide
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
Standard InChIKey VZZJRYRQSPEMTK-CALCHBBNSA-N
Standard InChI InChI=1S/C26H26F3N3O3/c1-16-14-32(15-17(2)34-16)24-12-9-20(13-30-24)31-25(33)23-6-4-5-22(18(23)3)19-7-10-21(11-8-19)35-26(27,28)29/h4-13,16-17H,14-15H2,1-3H3,(H,31,33)/t16-,17+
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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of LDE225 (NVP-LDE225,Erismodegib)

DescriptionLDE225 is a potent and selective antagonist of Smoothened (Smo) with IC50 values of 2.5 nM and 1.3 nM for human Hedgehog and mouse Hedgehog, respectively.
Targetshuman Hedgehogmouse Hedgehog    
IC502.5 nM1.3 nM    

Protocol

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.

Reacting condition

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

Application

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.

LDE225 (NVP-LDE225,Erismodegib) Dilution Calculator

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LDE225 (NVP-LDE225,Erismodegib) Molarity Calculator

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Preparing Stock Solutions of LDE225 (NVP-LDE225,Erismodegib)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.0597 mL 10.2987 mL 20.5973 mL 41.1946 mL 51.4933 mL
5 mM 0.4119 mL 2.0597 mL 4.1195 mL 8.2389 mL 10.2987 mL
10 mM 0.206 mL 1.0299 mL 2.0597 mL 4.1195 mL 5.1493 mL
50 mM 0.0412 mL 0.206 mL 0.4119 mL 0.8239 mL 1.0299 mL
100 mM 0.0206 mL 0.103 mL 0.206 mL 0.4119 mL 0.5149 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on LDE225 (NVP-LDE225,Erismodegib)

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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References on LDE225 (NVP-LDE225,Erismodegib)

Inhibition of Hedgehog signalling by NVP-LDE225 (Erismodegib) interferes with growth and invasion of human renal cell carcinoma cells.[Pubmed:25093491]

Br J Cancer. 2014 Sep 9;111(6):1168-79.

BACKGROUND: Multiple lines of evidence support that the Hedgehog (Hh) signalling has a role in the maintenance and progression of different human cancers. Therefore, inhibition of the Hh pathway represents a valid anticancer therapeutic approach for renal cell carcinoma (RCC) patients. NVP-LDE225 is a Smoothened (Smo) antagonist that induces dose-related inhibition of Hh and Smo-dependent tumour growth. METHODS: We assayed the effects of NVP-LDE225 alone or in combination with everolimus or sunitinib on the growth and invasion of human RCC models both in vitro and in vivo. To this aim, we used a panel of human RCC models, comprising cells with acquired resistance to sunitinib - a multiple tyrosine kinase inhibitor approved as a first-line treatment for RCC. RESULTS: NVP-LDE225 cooperated with either everolimus or sunitinib to inhibit proliferation, migration, and invasion of RCC cells even in sunitinib-resistant (SuR) cells. Some major transducers involved in tumour cell motility, including paxillin, were also efficiently inhibited by the combination therapy, as demonstrated by western blot and confocal microscopy assays. Moreover, these combined treatments inhibited tumour growth and increased animal survival in nude mice xenografted with SuR RCC cells. Finally, lung micrometastasis formation was reduced when mice were treated with NVP-LDE225 plus everolimus or sunitinib, as evidenced by artificial metastatic assays. CONCLUSIONS: Hedgehog inhibition by NVP-LDE225 plus sunitinib or everolimus bolsters antitumour activity by interfering with tumour growth and metastatic spread, even in SuR cells. Thus, this new evidence puts forward a new promising therapeutic approach for RCC patients.

Description

Erismodegib (Sonidegib) is a potent and selective Smoothened (Smo) antagonist with IC50s of 1.3 nM and 2.5 nM for mouse and human Smo, respectively.

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