产品
编 号:F751739
分子式:C61H76N12O7S
分子量:1121.4
产品类型
结构图
CAS No: 2378056-80-3
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产品详情
生物活性:
A947 is a potent and selective SMARCA2 proteolysis-targeting chimera molecule (PROTAC). A947 also is a potent and moderately selective SMARCA2 degrader. A947 has binding affinity to the SMARCA2 bromodomain with a Kd value of 93 nM. A947 can be used for the research of cancer.
体内研究:
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.Animal Model:SMARCA4-mutant NSCLC xenograft models
Dosage:40mg/kg
Administration:Intravenous , single-dose, 2 week; Intravenous , every other week, 30 days
Result:Rapidly reduced the tumor SMARCA2 protein levels and significant decreased the tumor growth.
体外研究:
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.