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PROTACATRdegrader-2 (Compound 8i) 作为一种有效的ATRPROTAC降解剂,能够在急性髓系白血病 (AML) 细胞 MV-4-11 和 MOLM-13 中分别以 DC50 值 22.9 nM 和 34.5 nM 降解 ATR。此外,PROTACATRdegrader-2 还能诱导细胞凋亡(apoptosis)并抑制 AML 细胞的增殖。在小鼠体内,该化合物示出了优良的药物代谢动力学属性及显著的抗AML肿瘤活性。 (Pink: ATRligand; Blue: E3 ligase ligand Lenalidomide; Black: linker)
PROTACATRdegrader-2 (Compound 8i) 作为一种有效的ATRPROTAC降解剂,能够在急性髓系白血病 (AML) 细胞 MV-4-11 和 MOLM-13 中分别以 DC50 值 22.9 nM 和 34.5 nM 降解 ATR。此外,PROTACATRdegrader-2 还能诱导细胞凋亡(apoptosis)并抑制 AML 细胞的增殖。在小鼠体内,该化合物示出了优良的药物代谢动力学属性及显著的抗AML肿瘤活性。 (Pink: ATRligand; Blue: E3 ligase ligand Lenalidomide; Black: linker)
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | 询价 | 待询 | |
50 mg | 询价 | 待询 |
产品描述 | PROTAC ATR degrader-2 (Compound 8i) serves as a PROTAC degrader targeting ATR, effectively degrading it in acute myeloid leukemia (AML) cell lines MV-4-11 and MOLM-13, with DC50 values of 22.9 and 34.5 nM, respectively. This compound induces apoptosis and inhibits the proliferation of AML cells. Additionally, PROTAC ATR degrader-2 demonstrates favorable pharmacokinetic properties and potent antitumor activity in a mouse model of AML. (Pink: ATR ligand; Blue: E3 ligase ligand Lenalidomide; Black: linker) [1] |
分子量 | 743.81 |
分子式 | C40H41N9O6 |
CAS No. | 3010273-12-5 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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