Erismodegib diphosphate Inhibitor

Name: Erismodegib diphosphate Inhibitor; MyBioSource
Brand: MyBioSource
SKU: MBS5755083
Availability: InStock
Rating: 5 (10 reviews)

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5755083

Erismodegib diphosphate is an effective and selective Smo antagonist (IC50: 1.3nM and 2.5nM for mouse and human Smo in a binding assay, respectively). More details

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Product Documentation

Sample Manual Insert View PDF

Testing Data View PDF

Certificate of Analysis (COA) View PDF

QC Report View PDF

Material Safety Data Sheet View PDF

Technical Datasheet View PDF

Protocol View PDF

Product Overview

Online Datasheet in PDF

Product Name

Erismodegib diphosphate, Inhibitor

Full Product Name

Erismodegib diphosphate

Product Synonym Names

Sonidegib diphosphate; LDE225 diphosphate; NVP-LDE 225 diphosphate

Form/Format

Solid. Powder

Purity/Purification

99.86%

Preparation and Storage

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

Molecular Weight

681.49

Solubility

DMSO: 99mg/mL (145.27mM)
H2O: 0.25mg/mL (0.37mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)

Formula

C26H32F3N3O11P2

SMILES

OP(O)(O)=O.OP(O)(O)=O.C[C@H]1CN(C[C@@H](C)O1)c1ccc(NC(=O)c2cccc(-c3ccc(OC(F)(F)F)cc3)c2C)cn1

CAS Number

1218778-77-8

Target & IC50

mSmo: ic50 1.3nM
hSmo: ic50 2.5nM

In Vitro

Erismodegib diphosphate is a weak base with a measured pKa of 4.2 and exhibits relatively poor aqueous solubility. Erismodegib diphosphate demonstrates dose-related antitumor activity after 10 days of oral administration of a suspension of the diphosphate salt, in the subcutaneous Ptch+/-p53-/- medulloblastoma allograft mouse model. Bone marrow cells and spleen cells from a subset of treated mice are transplanted into secondary recipient mice. Erismodegib diphosphate (5mg/kg/day; once daily) obviously inhibits tumor growth, corresponding to a T/C value of 33% (p<0.05 as compared to vehicle controls). Erismodegib affords 51 and 83% regression respectively when dosed at 10 and 20mg/kg/day qd [1]. Transplantation of either bone marrow (BM) or spleen cells from mice treated with Erismodegib diphosphate+ Nilotinib results in reduced white cell count (WCC) and reduces leukaemia development in secondary recipients compared to Erismodegib or Nilotinib alone[2].

Product Categories/Family for Erismodegib diphosphate, inhibitor

Stem Cells

Product References and Citations for Erismodegib diphosphate, inhibitor

Pan S, et al. Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist. ACS Med Chem Lett. 2010 Mar 16;1(3):130-4.
Pan S, et al. Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist. ACS Med Chem Lett. 2010 Mar 16;1(3):130-4.
Irvine DA, et al. Deregulated hedgehog pathway signaling is inhibited by the smoothened antagonist LDE225 (Sonidegib) in chronic phase chronic myeloid leukaemia. Sci Rep. 2016 May 9;6:25476.
Irvine DA, et al. Deregulated hedgehog pathway signaling is inhibited by the smoothened antagonist LDE225 (Sonidegib) in chronic phase chronic myeloid leukaemia. Sci Rep. 2016 May 9;6:25476.
Ma W, et al. Reduced Smoothened level rescued Abeta-induced memory deficits and neuronal inflammation in animal models of Alzheimer's disease. J Genet Genomics. 2018 May 20;45(5):237-246.
Ma W, et al. Reduced Smoothened level rescued Abeta-induced memory deficits and neuronal inflammation in animal models of Alzheimer's disease. J Genet Genomics. 2018 May 20;45(5):237-246.

Other Notes

Small volumes of Erismodegib diphosphate, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for Erismodegib diphosphate purchase

MBS5755083 is an inhibitor targeting Erismodegib diphosphate.