| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
BSJ-03-204 triTFA targets CDK4 (Cyclin-Dependent Kinase 4) and CDK6 (Cyclin-Dependent Kinase 6) for degradation via the ubiquitin-proteasome pathway [15L12-L14]. It is a heterobifunctional molecule with three components: a Palbociclib-derived ligand that binds to CDK4/6, a linker, and a ligand that recruits the E3 ubiquitin ligase Cereblon. By simultaneously binding both CDK4/6 and Cereblon, the PROTAC brings the kinase into proximity with the ubiquitin ligase, leading to its polyubiquitination and subsequent degradation by the proteasome.
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| ln Vitro |
On MCL cell lines, BSJ-03-204 triTFA (0.0001-100 μM; for 3 or 4 days) has strong anti-proliferative effects[1]. BSJ-03-204 triTFA (1 μM; for 1 day) has a strong G1 arrest inducing effect[1]. In WT cells, BSJ-03-204 triTFA (0.1–5 μM; for 4 hours) only causes CDK4/6 degradation; IKZF1/3 is not affected[1].
In vitro, BSJ-03-204 triTFA is a potent degrader of CDK4 and CDK6. It exhibits half-maximal inhibitory concentration (IC₅0) values of 26.9 nM for CDK4/D1 and 10.4 nM for CDK6/D1 in biochemical assays measuring kinase activity [15L14-L15]. The compound demonstrates high selectivity, as it does not induce the degradation of other Cereblon neo-substrates such as IKZF1 or IKZF3 [16L5-L6]. It shows anti-cancer activity in various CDK4/6-dependent cell lines. |
| ln Vivo |
Detailed in vivo activity data for BSJ-03-204 triTFA are not extensively reported in standard product literature. As a PROTAC molecule, its in vivo efficacy is typically evaluated in mouse xenograft models of cancer, such as breast cancer (e.g., MCF-7) or mantle cell lymphoma. Animals are administered the compound orally or intraperitoneally, and tumor growth inhibition (TGI) is measured. The favorable pharmacokinetic properties of the linker contribute to the molecule's bioavailability.
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| Enzyme Assay |
Binding studies for the CDK4/6-targeting warhead of this PROTAC are similar to those for Palbociclib. To confirm ternary complex formation, non-cellular assays such as FRET (Förster resonance energy transfer) or AlphaLISA (Amplified Luminescent Proximity Homogeneous Assay) can be used. In these systems, recombinant CDK4/6-Cyclin D protein is labeled with one tag, and Cereblon protein is labeled with another. When the PROTAC (BSJ-03-204 triTFA) is added, it bridges the two proteins, bringing the tags into close proximity, which generates a quantifiable signal. This assay confirms that the compound can physically link the target to the ligase.
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| Cell Assay |
For in vitro cellular assays, cancer cell lines that are sensitive to CDK4/6 inhibition (such as MCF-7 breast cancer cells or mantle cell lymphoma lines) are treated with various concentrations of BSJ-03-204 triTFA for 6-24 hours. The extent of CDK4 and CDK6 protein degradation is assessed by Western blotting of cell lysates using specific antibodies. The half-maximal degradation concentration (DC₅0) is calculated. Additionally, the effect on cell viability is measured using MTT or CellTiter-Glo assays to determine the anti-proliferative effect.
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| Animal Protocol |
In vivo studies for BSJ-03-204 triTFA are typically performed using a mouse xenograft model. For example, MCF-7 breast cancer cells are injected subcutaneously into immunodeficient mice to establish tumors. Once tumors reach a certain size, the PROTAC is administered intraperitoneally (IP) or orally (PO) at a specific dose (e.g., 10-50 mg/kg) on a daily or every-other-day schedule for 2-4 weeks. Tumor volumes are measured with calipers every 2-3 days to assess tumor growth inhibition (TGI). At the end of the study, tumors are excised and analyzed by Western blot to confirm CDK4/6 degradation.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) data for BSJ-03-204 triTFA are not detailed in standard product literature. However, as a PROTAC molecule, its PK properties, such as low oral bioavailability due to high molecular weight, poor membrane permeability, and rapid clearance, are generally considered a challenge. The TFA salt form is used to improve solubility and stability. For research use, the compound is typically administered via IP injection to maximize systemic exposure.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for BSJ-03-204 triTFA are not detailed in standard product documentation. As a CDK4/6 degrader and a PROTAC, its potential toxicities include on-target effects such as myelosuppression (neutropenia), which is a class effect of CDK4/6 inhibitors. However, a potential advantage of PROTACs is an improved safety profile, as they induce catalytic protein degradation rather than sustained occupancy. Standard research chemical safety precautions apply.
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| References |
[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.
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| Additional Infomation |
BSJ-03-204 triTFA has the molecular formula C4₉H₅1F₉N10O14 and a molecular weight of 1174.97 g/mol [16L20]. The CAS number is not listed. It appears as a solid. The compound is stored in lyophilized form at -20degC, where it is stable for up to 36 months. Once dissolved, it should be stored at -20degC and used within 1 month to prevent loss of potency [16L23-L26].
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| Molecular Formula |
C49H51F9N10O14
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| Molecular Weight |
1174.97
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| Related CAS # |
BSJ-03-204; 2349356-09-6
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| Appearance |
Light yellow to yellow solid
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| SMILES |
O=C1N(C2CCCC2)C3=NC(NC4=CC=C(N(CC5)CCN5CCCCNC(COC6=C(C(N7C(CCC8=O)C(N8)=O)=O)C(C7=O)=CC=C6)=O)C=N4)=NC=C3C(C)=C1C(C)=O.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~100 mg/mL (~85.11 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.13 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8511 mL | 4.2554 mL | 8.5109 mL | |
| 5 mM | 0.1702 mL | 0.8511 mL | 1.7022 mL | |
| 10 mM | 0.0851 mL | 0.4255 mL | 0.8511 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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