| Bioactivity | SIAIS562055 is a potent cereblon-based SOS1 PROTAC with a Kd of 95.9 nM. SIAIS562055 exhibits sustained degradation of SOS1 and inhibition of downstream ERK pathways. SIAIS562055 effectively blocked the binding of KRASG12C or KRASG12D to SOS1, with the IC50 values of 95.7 nM and 134.5 nM, respectively. SIAIS562055 exhibits potent anticancer activity. (Pink: SOS1 ligand (HY-168638); Black: linker (HY-W539874); Blue: E3 ligase ligand (HY-W076696))[1]. |
| Invitro | SIAIS562055 (10-1000 nM; 24 小时) 表现出持续降解 SOS1 和抑制下游 ERK 通路，具有优异的抗增殖活性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> SIAIS562055 相关抗体: Western Blot Analysis[1] Cell Line: |
| In Vivo | SIAIS562055（20-50 mg/kg；腹腔注射；每日；持续 3 周）在 KRAS 突变异种移植中表现出良好的抗肿瘤效力[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C49H62F3N7O5S |
| Molar Mass | 918.12 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Ziwei Luo, et al. Targeted Degradation of SOS1 Exhibits Potent Anticancer Activity and Overcomes Resistance in KRAS-Mutant Tumors and BCR-ABL-Positive Leukemia. Cancer Res. 2024 Oct 22. |