2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
CAS NO.：2378056-80-3 Product Name：A947 Synonyms： EINECS: Molecular Formula：C61H76N12O7S Molecular Weight：1121.40
Target:
Kd: 93 nM (SMARCA2), 65 nM (SMARCA4); DC50 for SMARCA2: 39 pM (in SW1573 cells)
In Vivo
A947 (i.v.; 40 mg/kg; single-dose, 2 week or every other week, 30 days) has active in SMARCA4-mutant NSCLC xenograft models in vivo.
In Vitro
A947 has binding affinity to the SMARCA2 and SMARCA4 bromodomains with Kd values of 93 nM and 65 nM, respectively.
A947 can potently degrade SMARCA2 in SW1573 cells with a DC50 value of 39 pM.
A947 (100 nM, 500 nM) mediates ubiquitination and degradation of SMARCA2/4.
A947 (0-500 nM) can inhibit growth of SMARCA4-mutant NSCLC cells.
Kinase Assay
Cell Assay
Animal Administration
References
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