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LDE225

Cat. No. M2338

LDE225 Structure

Synonym: NVP-LDE225, Erismodegib

Size Price Availability Quantity
10mg USD 75 In stock
50mg USD 220 In stock
100mg USD 380 In stock
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Quality Control
Biological Activity

LDE225 (NVP-LDE225, also known as Sonidegib or erismodegib) 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 485.5
Formula C26H26F3N3O3
CAS Number 956697-53-3
Purity 100.00%
Solubility DMSO 80 mg/mL
Ethanol 80 mg/mL
Storage at -20°C
References

NVP-LDE225, a potent and selective SMOOTHENED antagonist reduces melanoma growth in vitro and in vivo.
Jalili A, et al. PLoS One. 2013 Jul 30;8(7):e69064. PMID: 23935925.

Hedgehog inhibition with the orally bioavailable Smo antagonist LDE225 represses tumor growth and prolongs survival in a transgenic mouse model of islet cell neoplasms.
Fendrich V, et al. Ann Surg. 2011 Nov;254(5):818-23. PMID: 22042473.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LDE225, NVP-LDE225, Erismodegib supplier, Hedgehog, inhibitors

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