BSJ-03-204 triTFA
Based on 1 Customer Validation
BSJ-03-204 triTFA is a PROTAC-based CDK degrader derived from Palbociclib (HY-50767). BSJ-03-204 triTFA targets bovine CDK4/CCND1 and CDK6/CCND1 complexes with IC50 values of 26.9 nM and 10.4 nM, respectively. BSJ-03-204 triTFA also triggers ubiquitination and degradation of RB1, reduces pRb levels, thereby inducing G1 cell cycle arrest and exerting antiproliferative effects, as well as inducing time-dependent KLHL8 accumulation. BSJ-03-204 triTFA can be used in research related to pancreatic ductal adenocarcinoma, breast cancer, lung cancer, mantle cell lymphoma, and cloned bovine placental hyperplasia.
(Pink: Cdk6/cyclin D2 and CDK4 ligand (HY-50767); Blue: Cereblon ligand (HY-103596); Black: linker (HY-W007803)).
For research use only. We do not sell to patients.
- Purity : 99.87%
- Formula: C49H51F9N10O14
- Molecular Weight:1174.97
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
Cdk4/cyclin D1 26.9 nM (IC50) |
CDK6/cyclinD1 10.4 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | EC50 |
10.8 μM
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Stabilization of CDK4 in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
Stabilization of CDK4 in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
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33445986 |
| K562 | EC50 |
4.8 μM
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Stabilization of CDK6 in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
Stabilization of CDK6 in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
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33445986 |
| K562 | EC50 |
6.4 μM
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Stabilization of CRBN in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
Stabilization of CRBN in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
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33445986 |
| K562 | EC50 |
13.6 μM
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Stabilization of FECH in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
Stabilization of FECH in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
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33445986 |
| K562 | EC50 |
9.6 μM
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Stabilization of HNRNPDL in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
Stabilization of HNRNPDL in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
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33445986 |
| K562 | EC50 |
14.4 μM
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Stabilization of HNRNPUL1 in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
Stabilization of HNRNPUL1 in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
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33445986 |
| K562 | EC50 |
11.7 μM
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Stabilization of PIP4K2A in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
Stabilization of PIP4K2A in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
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33445986 |
| K562 | EC50 |
12.4 μM
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Stabilization of PLK1 in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
Stabilization of PLK1 in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
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33445986 |
| K562 | EC50 |
10.2 μM
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Stabilization of TIA1 in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
Stabilization of TIA1 in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
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33445986 |
| K562 | EC50 |
9.1 μM
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Stabilization of TIAL1 in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
Stabilization of TIAL1 in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
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33445986 |
| K562 | EC50 |
1.1 μM
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Destabilization of RB1 in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
Destabilization of RB1 in intact K562 cells measured via compressed cellular thermal shift assay mass spectrometry (CETSA MS) following 1 h incubation at 37°C.
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33445986 |
In Vitro
BSJ-03-204 triTFA (0.02-20 μM; 15 min) directly binds to and stabilizes CDK4, CDK6, CRBN, CSNK2A2, FECH, HNRNPDL, HNRNPUL1, PIP4K2A, PLK1, TIA1 and TIAL1 in lysed K562 cells, while destabilizing RB1, with EC50 values ranging from 0.3 μM to 10.0 μM[1].
BSJ-03-204 triTFA (0.02-20 μM; 1 h) induces degradation of CDK4 and CDK6 at lower concentrations and stabilizes them at 20 μM in intact K562 cells. It also stabilizes CRBN, FECH, HNRNPDL, HNRNPUL1, PIP4K2A, PLK1, TIA1 and TIAL1, and destabilizes RB1, with EC50 values ranging from 1.1 μM to 14.4 μM[1].
BSJ-03-204 triTFA (0.1-0.2 μM; 18-48 h) mediates the degradation of CDK4 and CDK6 in 1222 pancreatic ductal adenocarcinoma (PDAC) cells; at 18 h, it exhibits stronger activity against CDK4 than Palbo-PROTAC, while at 48 h, its degradative effect persists but is less potent than that of BSJ-02-162[2].
BSJ-03-204 triTFA (250 nM; 5 h) selectively degrades CDK4 and CDK6 in Molt4 cells, with no degradation of IKZF1 or IKZF3 observed[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PDAC 1222 cells
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Concentration:0.1-0.2 μM (18 h incubation); 0.1-0.2 μM (48 h incubation)
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Incubation Time:18 h; 48 h
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Result:Degraded CDK4 and CDK6 after 18 h incubation, showing greater potency for CDK4 degradation compared to Palbo-PROTAC.
Continued to degrade CDK4 and CDK6 after 48 h incubation, though exhibited less potency than BSJ-02-162 for degrading both kinases.
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Cell Line:Granta-519 mantle cell lymphoma (MCL) cells
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Concentration:1 µM
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Incubation Time:1 day
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Result:Induced pronounced loss of CDK4 and CDK6 protein levels.
Reduced levels of phosphorylated retinoblastoma (Rb).
Potently induced G1 cell cycle arrest.
Chemical Information
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Appearance Solid
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Molecular Weight 1174.97
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Formula C49H51F9N10O14
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Color Light yellow to yellow
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (85.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.13 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.13 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (289 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.8511 mL | 4.2554 mL | 8.5109 mL | 21.2771 mL |
| 5 mM | 0.1702 mL | 0.8511 mL | 1.7022 mL | 4.2554 mL | |
| 10 mM | 0.0851 mL | 0.4255 mL | 0.8511 mL | 2.1277 mL | |
| 15 mM | 0.0567 mL | 0.2837 mL | 0.5674 mL | 1.4185 mL | |
| 20 mM | 0.0426 mL | 0.2128 mL | 0.4255 mL | 1.0639 mL | |
| 25 mM | 0.0340 mL | 0.1702 mL | 0.3404 mL | 0.8511 mL | |
| 30 mM | 0.0284 mL | 0.1418 mL | 0.2837 mL | 0.7092 mL | |
| 40 mM | 0.0213 mL | 0.1064 mL | 0.2128 mL | 0.5319 mL | |
| 50 mM | 0.0170 mL | 0.0851 mL | 0.1702 mL | 0.4255 mL | |
| 60 mM | 0.0142 mL | 0.0709 mL | 0.1418 mL | 0.3546 mL | |
| 80 mM | 0.0106 mL | 0.0532 mL | 0.1064 mL | 0.2660 mL |
BSJ-03-204 triTFA Related Classifications
HY-136250A Related Classifications
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