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编 号:F751445
分子式:C57H76ClN10O7PS
分子量:1111.77
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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.

体外研究:
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.SIAIS117 (0-500 nM, 24 h) inhibits the phosphorylation of ALK and STAT3.SIAIS117 inhibits the growth of G1202R-mutant ALK cell line and degrades G1202R-ALK protein.SIAIS117 (100 nM, 24 h) causes sustained degradation of ALK protein in SR cells.
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