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HhAntag

Cat No.
CEI-1360
Product Overview
HhAntag is a Hedgehog signaling antagonist. Ligand-dependent activation of the Hedgehog (Hh) signaling pathway has been associated with tumorigenesis in a number of human tissues.
CAS No.
496794-70-8
Molecular Weight
450.92
Purity
0.9895
Storage
Store at -20°C
Targets
GLI1
IC50
from 2 μM to >30 μM
Molecular Formula
C24H23ClN4O3
Chemical Name
N-[4-chloro-3-[6-(dimethylamino)-1H-benzimidazol-2-yl]phenyl]-3,5-dimethoxybenzamide
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
In vitro
HhAntag has been evaluated for its effect on Hh pathway across a large panel of cancer cell lines. HhAntag demonstrated to be around 10-times more potent than cyclopamine at inhibiting the activity of Hh pathway. A range of cellular sensitivities to HhAntag was observed with IC50 values for growth inhibition ranging from ~2 μM to >30 μM. In contrast to previous reports, no tissue specificity of in vitro sensitivity to HhAntag was observed.
In vivo
Oral administration of HhAntag to mice with primary human xenografts resulted in significant growth delay in both pancreatic and colon adenocarcinoma models, with average tumour growth inhibitions of 29% and 48%, respectively. Moreover, the HhAntag doses required to inhibit the tumor growth were similar to the doses required to fully inhibit endogenous Hh target genes in tumour stroma or in surrogate normal tissues, indicating that such growth inhibition was a specific consequence of Hh inhibition.
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