SIAIS117

发表于由

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。

SIAIS117 

SIAIS117 是一种有效的 Brigatinib-PROTAC 降解剂。SIAIS117 是一种基于Brigatinib 和 VHL-1 结合的 ALK PROTAC。SIAIS117 能有效降解 ALK G1202R 点突变SIAIS117可阻断 SR 和 H2228 癌细胞株的生长。SIAIS117 具有潜在的小细胞肺癌的抗增殖能力。

SIAIS117

SIAIS117 Chemical Structure

CAS No. : 2353494-84-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SIAIS117 is a potent Brigatinib-PROTAC degrader. SIAIS117 is a ALK PROTAC based on Brigatinib and VHL-1 conjunction. SIAIS117 can degrade ALK G1202R point mutation effectively. SIAIS117 blocks the growth of SR and H2228 cancer cell lines. SIAIS117 has the potentially anti-proliferation ability of small cell lung cancer[1].

体外研究
(In Vitro)

SIAIS117 (0-10 μM, 72 h) inhibits SR, H2228, NCI-H69 and NCI-H1688 cell growth, with IC50 values of 1.7, 46, 799, and 259 nM, respectively[1].
SIAIS117 (0-500 nM, 24 h) inhibits the phosphorylation of ALK and STAT3[1].
SIAIS117 inhibits the growth of G1202R-mutant ALK cell line and degrades G1202R-ALK protein[1].
SIAIS117 (100 nM, 24 h) causes sustained degradation of ALK protein in SR cells[1].

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

Cell Proliferation Assay

Cell Line: NSCLC cell line H2228, Small cell lung cancer cell lines (NCI-H69, NCI-H1688)[1]
Concentration: 0-10 μM
Incubation Time: 72 h
Result: Inhibited cell growth with an about two folds lower IC50 value (46 nM) comparing to SIAIS117NC (114 nM). Showed a good growth inhibition effect on NCI-H69 and NCI-H1688 cell line, with IC50 values of 799 and 259 nM, respectively.

Western Blot Analysis

Cell Line: SR, H2228[1]
Concentration: 0, 1, 10, 50, 100, 500 nM
Incubation Time: 24 h
Result: Inhibited all of the phosphorylation of ALK at 10 nM and inhibited pSTAT3 in SR cell, degraded ALK proteins at the concentration starting from 50 nM in H2228 cell, and significantly downregulated UCK2 and GAK. Caused sustained degradation of ALK protein in SR cells.

分子量

1111.77

Formula

C57H76ClN10O7PS
CAS 号

2353494-84-3
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]. Sun N, Ren C, Kong Y, et al. Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance. Eur J Med Chem. 2020;193:112190.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务