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LDE225 (Sonidegib) diphosphate

Cat. No. M4841
LDE225 (Sonidegib) diphosphate Structure
Synonym:

NVP-LDE225; Erismodegib; Sonidegib diphosphate

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 70  USD70 In stock
5mg USD 50  USD50 In stock
10mg USD 60  USD60 In stock
50mg USD 130  USD130 In stock
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Quality Control & Documentation
Biological Activity

LDE225 (Sonidegib) diphosphate is a potent and selective Hedgehog signaling pathway inhibitor (Smoothened antagonist) reduces melanoma growth in vitro and in vivo. NVP-LDE225 was potent in reducing cell proliferation and inducing tumor growth arrest in vitro and in vivo, respectively.Pharmacologic inhibition of BRAF(V600E) in human melanoma cell lines resulted in decreased expression of GLI1 thus demonstrating interaction of SHH-GLI and MAPK pathways. Inhibition of SHH-GLI pathway by the novel small molecule inhibitor of smoothened NVP-LDE225 was followed by inhibition of cell growth and induction of apoptosis in human melanoma cell lines, interestingly with both BRAF(V600E) and BRAF(Wild Type) status.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.

Customer Product Validations & Biological Datas
Source BMC Cancer (2017). Figure 4. LDE225
Method western blot
Cell Lines BALB/c nude mice
Concentrations 80 mg/kg
Incubation Time 41 day
Results Western blotting showed increased amounts of GLI1 in tumors from animals treated with 177Lu-octreotate monotherapy and combination treatment, and increased amounts of GLI2 in tumors from the combination therapy group, compared with controls
Chemical Information
Molecular Weight 681.49
Formula C26H32F3N3O11P2
CAS Number 1218778-77-8
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Pan S, et al. ACS Med Chem Lett. Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist.

[2] Jalili A, et al. PLoS One. NVP-LDE225, a potent and selective SMOOTHENED antagonist reduces melanoma growth in vitro and in vivo.

[3] Fendrich V, et al. Ann Surg. Hedgehog inhibition with the orally bioavailable Smo antagonist LDE225 represses tumor growth and prolongs survival in a transgenic mouse model of islet cell neoplasms.

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Keywords: LDE225 (Sonidegib) diphosphate, NVP-LDE225; Erismodegib; Sonidegib diphosphate supplier, Smo, inhibitors, activators


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