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首页-抗体药物偶连体和PROTACs-PROTAC-SMD-3236
SMD-3236

Chemical Structure : SMD-3236

CAS No.: 3033586-31-8

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SMD-3236 (SMD3236)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 1095.85
分子式 C61H75ClN10O5S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(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

参考文献

1. Yang L, et al. J Med Chem. 2025 Jan 2. doi: 10.1021/acs.jmedchem.4c01904.

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