Chemical Structure : SMD-3040
CAS No.: 3033109-92-8
Catalog No.: PC-23675Not For Human Use, Lab Use Only.
SMD-3040 is a highly potent, exceptionally selective SMARCA2 PROTAC degrader with DC50 of 12 nM and Dmax = 96% in Hela cells, >500-fold selectivity over SMARC4.
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SMD-3040 is a highly potent, exceptionally selective SMARCA2 PROTAC degrader with DC50 of 12 nM and Dmax = 96% in Hela cells, >500-fold selectivity over SMARC4.
SMD-3040 achieved a DC50 value of 35 nM and a Dmax value of 98% for SMARCA2 in SK-Mel-28 SMARCA4 WT cell line.
SMD-3040 achieved DC50 values of 20 and 63 nM in SK-Mel-5 and H838 cell lines, respectively, with Dmax values of 94 and 90%, respectively.
SMD-3040 is selective in cell growth inhibition of SMARCA4-deficient cancer cell lines over SMARCA4 wild-type cancer cell lines.
SMD-3040 exhibits strong tumor growth inhibition in two SMARCA4-deficient xenograft models at well-tolerated dose schedules.
M.Wt | 943.23 | |
Formula | C52H66N10O5S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
(2S,4R)-1-((S)-2-((1r,4S)-4-((7-(4-(3-Amino-6-(2-hydroxyphenyl)pyridazin-4-yl)-1H-pyrazol-1-yl)-2-azaspiro[3.5]nonan-2-yl)methyl)cyclohexane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide |
1. Lin Yang, et al. J Med Chem. 2023 Aug 10;66(15):10761-10781.
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