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MSC-5046

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

M.Wt 481.44
Formula C24H18F3N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(2-(acrylamidomethyl)-3-fluoro-4-(4-fluorophenoxy)benzyl)-6-fluoroimidazo[1,2-a]pyrimidine-3-carboxamide

References

1. Carswell E, et al. Bioorg Med Chem Lett. 2024 Oct 4:129981.

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