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SMD-3236是一种基于SMARCA配体和VHL-1配体设计的PRAOTAC降解剂,专门针对SMARCA2,展示了体内的长效抗肿瘤活性。SMARCA2是SMARCA4缺陷癌细胞中的合成致死靶点,SMD-3236对SMARCA2的降解选择性是SMARCA4的2000倍,DC50< 1 nM,Dmax>95%。SMD-3236可诱导肿瘤组织的SMARCA2缺失,同时保留SMARCA4蛋白,并在H838 smarca4缺陷人类癌症异种移植模型中抑制肿瘤生长。SMD-3236由靶蛋白配体(red part) SMI-1074、 PROTAC linker (black part) (trans-4-Ethynylcyclohexyl) methyl methanesulfonate 和E3连接酶配体(blue part)SMARCA2 ligand-14组成,其中E3连接酶配体和linker构成偶联物E3LigaseLigand-linker Conjugate 159。
SMD-3236是一种基于SMARCA配体和VHL-1配体设计的PRAOTAC降解剂,专门针对SMARCA2,展示了体内的长效抗肿瘤活性。SMARCA2是SMARCA4缺陷癌细胞中的合成致死靶点,SMD-3236对SMARCA2的降解选择性是SMARCA4的2000倍,DC50< 1 nM,Dmax>95%。SMD-3236可诱导肿瘤组织的SMARCA2缺失,同时保留SMARCA4蛋白,并在H838 smarca4缺陷人类癌症异种移植模型中抑制肿瘤生长。SMD-3236由靶蛋白配体(red part) SMI-1074、 PROTAC linker (black part) (trans-4-Ethynylcyclohexyl) methyl methanesulfonate 和E3连接酶配体(blue part)SMARCA2 ligand-14组成,其中E3连接酶配体和linker构成偶联物E3LigaseLigand-linker Conjugate 159。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | 待询 | 期货 | |
50 mg | 待询 | 期货 |
产品描述 | SMD-3236 is a PRAOTAC degrader targeting SMARCA2, designed using SMARCA ligand and VHL-1 ligand, and exhibits prolonged anti-tumor activity in vivo. SMARCA2 acts as a synthetic lethal target in cancer cells lacking SMARCA4, with SMD-3236 showing 2000-fold selectivity for SMARCA2 over SMARCA4, having a DC50 of less than 1 nM and a Dmax of over 95%. In the human cancer xenograft models deficient in SMARCA4, notably the H838 model, SMD-3236 effectively induces loss of SMARCA2 in tumor tissue while sparing the SMARCA4 protein, thereby inhibiting tumor growth. The compound consists of a target protein ligand (red part) SMI-1074, a PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate, and an E3 ligase ligand (blue part) SMARCA2 ligand-14, forming the E3LigaseLigand-linker Conjugate 159. |
分子量 | 1095.83 |
分子式 | C61H75ClN10O5S |
CAS No. | 3033586-31-8 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
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