SIAIS164018

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SIAIS164018 

SIAIS164018 是一种基于 PROTAC 的 ALK 和 EGFR 降解剂，由 Brigatinib 设计，对 ALK 和 ALK G1202R 的 IC50 分别为 2.5 nM 和 6.6 nM。SIAIS164018 强烈抑制癌细胞迁移和侵袭，引起细胞阻滞在 G1 期，诱导细胞凋亡 (apoptosis)。SIAIS164018表现出比 Brigatinib 更好的性能。

SIAIS164018

SIAIS164018 Chemical Structure

CAS No. : 2353492-68-7

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生物活性

SIAIS164018 is a PROTAC-based ALK and EGFR degrader, which is designed from Brigatinib, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib[1].

IC50 & Target

IC50: 2.5 nM (ALK), 6.6 nM (ALK G1202R)[1]
体外研究
(In Vitro)

SIAIS164018 significantly inhibits SR cell proliferation with an IC50 value of 2 nM[1].
SIAIS164018 shows better cell proliferation inhibition than Brigatinib does in ALK (G1202R) over-expressing 293T and EGFR expressing H1975 cell lines with IC50s 21 and 42 nM, respectively[1].
SIAIS164018 (100 nM; 24 or 48 h) induces a significant G1 cell cycle arrest in ALK-negative Calu-1 and MDA-MB-231 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

883.33

Formula

C43H48ClN10O7P
CAS 号

2353492-68-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Ren C, et al. Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile. J Med Chem. 2021 Jul 8;64(13):9152-9165.

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