Chemical Structure : SMD-3236
CAS No.:
3033586-31-8
SMD-3236
(SMD3236)
Catalog No.: PC-23674Not For Human Use, Lab Use Only.
SMD-3236 is a highly potent, exceptionally selective SMARCA2 PROTAC degrader with DC50 of 0.5 nM and Dmax = 96% in H838 NSCLC cells, >2000-fold selectivity over SMARC4.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
SMD-3236 is a highly potent, exceptionally selective SMARCA2 PROTAC degrader with DC50 of 0.5 nM and Dmax = 96% in H838 NSCLC cells, >2000-fold selectivity over SMARC4.
SMD-3236 binds to SMARCA2 and SMARCA4 with IC50 values of 42.2 and 60.0 nM, respectively, in TR-FRET binding assays.
SMD-3236 demonstrates GI50 values ranging from 1.5 to 9.8 nM and Imax values spanning 71–95% against 5 SMARCA4-deficient cancer cell lines, demonstrates >1000-fold selectivity over cancer cell lines carrying wild-type SMARCA4.
SMD-3236 (10 mg/kg via the tail vein injection) induce SMARCA2 degradation in the H838 SMARCA4-deficient xenograft tumor model in mice.
SMD-3236 (10 and 30 mg/kg intravenously for 3 weeks) effectively inhibits tumor growth in the H838 xenograft tumor model in SCID mice.
Physicochemical Properties
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M.Wt
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1095.85
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Formula
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C61H75ClN10O5S
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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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(2S,4R)-1-((S)-2-(4-((1r,4S)-4-((4-(4'-chloro-5'-oxo-5'H-spiro[cyclohexane-1,7'-indolo[1,2-a]quinazolin]-10'-yl)piperidin-1-yl)methyl)cyclohexyl)-1H-1,2,3-triazol-1-yl)-3,3-dimethylbutanoyl)-4-hydroxy-N-((R)-1-(4-(4-methylthiazol-5-yl)phenyl)-2-morpholinoethyl)pyrrolidine-2-carboxamide
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References
1. Yang L, et al. J Med Chem. 2025 Jan 2. doi: 10.1021/acs.jmedchem.4c01904.
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