Chemical Structure : MSC-5046
CAS No.:
MSC-5046
(MSC5046)
Catalog No.: PC-23231Not For Human Use, Lab Use Only.
MSC-5046 is a potent, selective, reversible TEAD1 inhibitor with EC50 of 58 nM in TEAD-reporter assay in SK-Hep-1 cells, shows viability affect in NCI-H226 cell line with EC50 of 12 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
MSC-5046 is a potent, selective, reversible TEAD1 inhibitor with EC50 of 58 nM in TEAD-reporter assay in SK-Hep-1 cells, shows viability affect in NCI-H226 cell line with EC50 of 12 nM.
MSC-5046 shows cellular palmitoylation inhibition of TEAD1 in HEK-293 cells, but not TEAD2, TEAD3 and TEAD4.
MSC-5046 has a favourable in vitro profile in a suite of cellular assays with a good correlation between TEAD-reporter, on-target NCI-H226 viability and TEAD regulated target gene Cyr61 biomarker modulation in both NCI-H226 and SK-HEP-1 cell lines.
Physicochemical Properties
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M.Wt
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481.44
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Formula
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C24H18F3N5O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(2-(acrylamidomethyl)-3-fluoro-4-(4-fluorophenoxy)benzyl)-6-fluoroimidazo[1,2-a]pyrimidine-3-carboxamide
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References
1. Carswell E, et al. Bioorg Med Chem Lett. 2024 Oct 4:129981.
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