常用名：SIAIS164018 hydrochloride

产品描述 SIAIS164018 hydrochloride is a PROTAC-based degrader targeting ALK and EGFR, exhibiting IC50 values of 2.5 nM for ALK and 6.6 nM for ALK G1202R. It effectively suppresses cancer cell migration and invasion, induces G1 cell cycle arrest, and promotes apoptosis, demonstrating superior properties compared to Brigatinib [1].

体外活性

SIAIS164018 hydrochloride inhibits SR cell proliferation significantly at 0-1 μM for 16 hours. At concentrations of 0-100 nM and a treatment time of 72 hours, SIAIS164018 hydrochloride exhibits a greater inhibitory effect on cell proliferation in 293T cells overexpressing ALK (G1202R) and H1975 cells expressing EGFR compared to Brigatinib. At a concentration of 100 nM, SIAIS164018 hydrochloride induces significant G1 phase cell cycle arrest in ALK-negative Calu-1 and MDA-MB-231 cell lines within 24 or 48 hours. In a concentration range of 0.01-1000 nM and a treatment time of 16 hours, SIAIS164018 hydrochloride downregulates the protein expression levels of FAK, PYK2, FER, RSK1, and GAK in both ALK-positive SR cell line and ALK-negative Calu-1 cell line.

分子量 919.79

分子式 C43H49Cl2N10O7P

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

PROteolysis TArgeting Chimeras (PROTACs) 通过将靶蛋白和 E3 连接酶结合起来，从而“劫持”细胞的泛素-蛋白酶体系统（UPS）来实现蛋白质的降解。由于 PROTACs 只需具有高选择性地结合其靶标（而不是抑制靶蛋白的酶活性），目前有许多努力将先前无效的抑制剂分子改造为 PROTACs，用作下一代药物。

产地：西安

用途：科研

厂家：西安齐岳生物科技有限公司

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