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SMARCA2-IN-8(Compound 13)是针对SWI/SNF染色质重塑复合物中的SMARCA2(Brahma 同源物,BRM)和SMARCA4(Brahma 相关基因1,BRG1)的口服有效抑制剂,其IC50值分别为5 nM和6 nM.此化合物能有效抑制携带SMARCA2突变的癌细胞SKMEL5的增殖,AAC50为5 nM,并能下调依赖SMARCA2的KRT80基因的表达,AAC50为10 nM.在小鼠模型中,SMARCA2-IN-8展现出抗肿瘤活性以及良好的药物代谢动力学属性.
SMARCA2-IN-8(Compound 13)是针对SWI/SNF染色质重塑复合物中的SMARCA2(Brahma 同源物,BRM)和SMARCA4(Brahma 相关基因1,BRG1)的口服有效抑制剂,其IC50值分别为5 nM和6 nM.此化合物能有效抑制携带SMARCA2突变的癌细胞SKMEL5的增殖,AAC50为5 nM,并能下调依赖SMARCA2的KRT80基因的表达,AAC50为10 nM.在小鼠模型中,SMARCA2-IN-8展现出抗肿瘤活性以及良好的药物代谢动力学属性.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | 询价 | 10-14周 | |
50 mg | 询价 | 10-14周 |
产品描述 | SMARCA2-IN-8 (Compound 13) is an orally effective inhibitor targeting the SWI/SNF chromatin remodeling complexes SMARCA2 (also known as Brahma homolog, BRM) and SMARCA4 (also known as Brahma-related gene 1, BRG1), with IC50 values of 5 nM and 6 nM respectively. This compound inhibits the proliferation of SMARCA2-mutant SKMEL5 cancer cells with an AAC50 of 5 nM and downregulates the expression of the SMARCA2-dependent gene KRT80, showing an AAC50 of 10 nM. Additionally, SMARCA2-IN-8 demonstrates antitumor efficacy and favorable pharmacokinetic properties in mice. |
分子量 | 303.26 |
分子式 | C10H8F3N5OS |
CAS No. | 2270875-93-7 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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