产品
编 号：F751444
分子式：C43H48ClN10O7P
分子量：883.33
分子式：C43H48ClN10O7P
分子量：883.33
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CAS No: 2353492-68-7
产品详情
生物活性：
SIAIS164018 is a PROTAC-based ALK and EGFR degrader, 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 (HY-12857).
体外研究：
SIAIS164018 (0-1 μM; 16 h) significantly inhibits SR cell proliferation.SIAIS164018 (0-100 nM; 72 h) shows better cell proliferation inhibition than Brigatinib does in ALK (G1202R) over-expressing 293T and EGFR expressing H1975 cell lines.SIAIS164018 (100 nM; 24 or 48 h) induces a significant G1 cell cycle arrest in ALK-negative Calu-1 and MDA-MB-231 cells.SIAIS164018 (0.01-1000 nM; 16h) down-regulates the protein level of FAK, PYK2, FER, RSK1, and GAK in ALK-positive SR and ALK-negative Calu-1 cell lines.
SIAIS164018 is a PROTAC-based ALK and EGFR degrader, 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 (HY-12857).
体外研究：
SIAIS164018 (0-1 μM; 16 h) significantly inhibits SR cell proliferation.SIAIS164018 (0-100 nM; 72 h) shows better cell proliferation inhibition than Brigatinib does in ALK (G1202R) over-expressing 293T and EGFR expressing H1975 cell lines.SIAIS164018 (100 nM; 24 or 48 h) induces a significant G1 cell cycle arrest in ALK-negative Calu-1 and MDA-MB-231 cells.SIAIS164018 (0.01-1000 nM; 16h) down-regulates the protein level of FAK, PYK2, FER, RSK1, and GAK in ALK-positive SR and ALK-negative Calu-1 cell lines.
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