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LY2940680

Cat No.
CEI-1412
Description
LY2940680 is a potent inhibitor of Smoothened (Smo) receptor and Hedgehog (Hh) signaling.
Product Overview
LY2940680 is a selective inhibitor of Smo receptor and thus inhibits Hh signaling pathway. Smoothened(Smo) receptor is a member of class F G protein-coupled receptors, which plays an important role in the main transducer of the Hedgehog (Hh) signaling pathway that implicated in a wide range of developmental and adult processes. LY2940680 is a potent Smo receptor inhibitor that binds mostly to extracelluar loops and has a different functioning site with the reported Smo receptor inhibitor SANT-1 which binds to 7TM. When tested with 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 inhibited cell proliferation. Many studies have shown that Hh signaling pathway plays a pivotal role in CSCs and Hh inhibition caused many aspects of transformation attributed to CSCs. In patients with basal cell carcinoma and medulloblastoma, LY2940680 showed good efficacy as a monotherapy.
CAS No.
1258861-20-9
Molecular Weight
512.5
Purity
0.98
Storage
Store at-20°C
Targets
Hedgehog/SMO
Molecular Formula
C26H24F4N6O
Chemical Name
4-fluoro-N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-2-(trifluoromethyl)benzamide
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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