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LY2940680

Cat. No. M2110
LY2940680 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 220 In stock
50mg USD 500 In stock
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Quality Control
Biological Activity

LY2940680 is a Hedgehog inhibitor in clinical trials. LY2940680 binds to the Smo receptor and potently inhibits Hh signaling. LY2940680 inhibits cancer growth in cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib. LY2940680 induces Caspase-3 activity and reduces proliferation by immunohistochemistry analysis of medulloblastoma tumors. LY2940680 is currently being tested in phase I trials for people with a range of solid tumors.

Customer Product Validations & Biological Datas
Source PLoS One (2015). Figure 3. LY2940680
Method MTS assay
Cell Lines CCA Cell
Concentrations 50 μM
Incubation Time 72 h
Results In contrast, Vismodegib, a small-molecule antagonist of Smoothened and LY2940680, a small-molecule antagonist of the smoothened receptor, showed a slight inhibitory effect on cell proliferation without differences between mucin-(IC50: Vismodecib = 61.7 ± 1.4 μM, LY2940680 = 49.8 ± 4.5 μM) and mixed-CCA (IC50: Vismodecib = 81.6 ± 14.8 μM, LY2940680 = 61.2 ± 21.1 μM).
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 512.5
Formula C26H24F4N6O
CAS Number 1258861-20-9
Purity 99.70%
Solubility Ethanol 2 mg/mL
Storage at -20°C
References

Investigational Notch and Hedgehog inhibitors--therapies for cardiovascular disease.
Redmond EM, et al. Expert Opin Investig Drugs. 2011 Dec;20(12):1649-64. PMID: 22007748.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LY2940680 supplier, Hedgehog, inhibitors

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