| Bioactivity | SIAIS164018 hydrochloride 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 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857)[1]. |
| Invitro | SIAIS164018 (0-1 μM；16 小时) hydrochloride 显着抑制 SR 细胞增殖[1]。SIAIS164018 (0-100 nM；72 h) hydrochloride 在过表达 ALK (G1202R) 的 293T 和表达 EGFR 的 H1975 细胞系中，显示出比 Brigatinib 更好的细胞增殖抑制作用[1]。SIAIS164018 (100 nM；24 或 48 小时) hydrochloride 可在 ALK 阴性 Calu-1 和 MDA-MB-231 细胞中诱导显着的 G1 细胞周期停滞[1]。SIAIS164018 (0.01-1000 nM；16 小时) hydrochloride 下调 ALK 阳性 SR 细胞系和 ALK 阴性 Calu-1 细胞系中 FAK、PYK2、FER、RSK1 和 GAK 的蛋白水平[1]。 Cell Proliferation Assay[1] Cell Line: |
| Name | SIAIS164018 hydrochloride |
| Formula | C43H49Cl2N10O7P |
| Molar Mass | 919.79 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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. |
SIAIS164018 hydrochloride
CAS: F: C43H49Cl2N10O7P W: 919.79
SIAIS164018 hydrochloride is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK
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