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BSJ-03-204 triTFA is a potent and selective Cereblon- and CDK-targeted PROTAC (PROteolysis TArgeting Chimera) featuring Palbociclib-based ligands for the degradation of CDK4/6. It exhibits IC50 values of 26.9 nM for CDK4/D1 and 10.4 nM for CDK6/D1, indicating strong inhibitory capabilities. Notably, it spares IKZF1/3 from degradation and possesses anti-cancer activity [1].
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| 5 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | BSJ-03-204 triTFA is a potent and selective Cereblon- and CDK-targeted PROTAC (PROteolysis TArgeting Chimera) featuring Palbociclib-based ligands for the degradation of CDK4/6. It exhibits IC50 values of 26.9 nM for CDK4/D1 and 10.4 nM for CDK6/D1, indicating strong inhibitory capabilities. Notably, it spares IKZF1/3 from degradation and possesses anti-cancer activity [1]. |
| In vitro | BSJ-03-204 triTFA, at concentrations ranging from 0.0001 to 100 μM administered for 3 or 4 days, exhibits potent anti-proliferative effects on MCL cell lines [1]. Additionally, a 1 μM dose for 1 day strongly induces G1 phase arrest [1]. When applied at 0.1 to 5 μM for a period of 4 hours, BSJ-03-204 triTFA selectively leads to the degradation of CDK4/6 in WT cells without affecting IKZF1/3 [1]. |
| Molecular Weight | 1174.97 |
| Formula | C49H51F9N10O14 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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