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LDE225 Diphosphate

Cat. No. M4841
LDE225 Diphosphate Structure

NVP-LDE225, Erismodegib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 50 In stock
10mg USD 75 In stock
50mg USD 180 In stock
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Quality Control
Biological Activity

LDE225 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
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 681.49
Formula C26H32F3N3O11P2
CAS Number 1218778-77-8
Purity >99%
Solubility DMSO
Storage at -20°C

Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist.
Pan S, et al. ACS Med Chem Lett. 2010 Mar 16;1(3):130-4. PMID: 24900187.

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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Abmole Inhibitor Catalog 2017

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

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