| Bioactivity | SIAIS164018 is a PROTAC-based ALK and EGFR degrader, which is designed from Brigatinib (HY-12857), 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]. |
| Invitro | SIAIS164018 (0-1 μM; 16 h) significantly inhibits SR cell proliferation[1].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[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].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[1]. Cell Proliferation Assay[1] Cell Line: |
| Name | SIAIS164018 |
| CAS | 2353492-68-7 |
| Formula | C43H48ClN10O7P |
| Molar Mass | 883.33 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
SIAIS164018
CAS: 2353492-68-7 F: C43H48ClN10O7P W: 883.33
SIAIS164018 is a PROTAC-based ALK and EGFR degrader, which is designed from Brigatinib (HY-12857), with IC50 value of 2.
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This product is for research use only, not for human use. We do not sell to patients.