Bioactivity | BSJ-03-204 triTFA is a PROTAC connected by ligands for Cereblon and CDK. BSJ-03-204 triTFA is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 triTFA does not induce IKZF1/3 degradation and has anti-cancer activity[1]. |
Invitro | BSJ-03-204 triTFA (0.0001-100 μM; for 3 or 4 days) has potent anti-proliferative effects on MCL cell lines[1]. BSJ-03-204 triTFA (1 μM; for 1 day) potently induces a G1 arrest[1]. BSJ-03-204 triTFA (0.1-5 μM; for 4 hours) only resultes in degradation of CDK4/6 in WT cells, not IKZF1/3[1]. 0 --> BSJ-03-204 triTFA 相关抗体: |
Name | BSJ-03-204 triTFA |
Formula | C49H51F9N10O14 |
Molar Mass | 1174.97 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. Baishan Jiang, et al. Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6. Angew Chem Int Ed Engl. 2019 May 6;58(19):6321-6326. |