BSJ-03-204
Based on 1 Customer Validation
BSJ-03-204 is a PROTAC-based CDK degrader derived from Palbociclib (HY-50767). BSJ-03-204 targets bovine CDK4/CCND1 and CDK6/CCND1 complexes with IC50 values of 26.9 nM and 10.4 nM, respectively. BSJ-03-204 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 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 : 99.76%
- CAS No.: 2349356-09-6
- Formula: C43H48N10O8
- Molecular Weight:832.90
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Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
- Protocols
- 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) |
MCE Validation Data
In Vitro
BSJ-03-204 (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 (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 (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 (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. Further protocols information, click here.
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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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CAS No. 2349356-09-6
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Appearance Solid
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Molecular Weight 832.90
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Formula C43H48N10O8
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (120.06 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 (protect from light). 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 (protect from light). 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.
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 (protect from light)
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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
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BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
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Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (283 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 (protect from light). 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 |
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| DMSO | 1 mM | 1.2006 mL | 6.0031 mL | 12.0062 mL | 30.0156 mL |
| 5 mM | 0.2401 mL | 1.2006 mL | 2.4012 mL | 6.0031 mL | |
| 10 mM | 0.1201 mL | 0.6003 mL | 1.2006 mL | 3.0016 mL | |
| 15 mM | 0.0800 mL | 0.4002 mL | 0.8004 mL | 2.0010 mL | |
| 20 mM | 0.0600 mL | 0.3002 mL | 0.6003 mL | 1.5008 mL | |
| 25 mM | 0.0480 mL | 0.2401 mL | 0.4802 mL | 1.2006 mL | |
| 30 mM | 0.0400 mL | 0.2001 mL | 0.4002 mL | 1.0005 mL | |
| 40 mM | 0.0300 mL | 0.1501 mL | 0.3002 mL | 0.7504 mL | |
| 50 mM | 0.0240 mL | 0.1201 mL | 0.2401 mL | 0.6003 mL | |
| 60 mM | 0.0200 mL | 0.1001 mL | 0.2001 mL | 0.5003 mL | |
| 80 mM | 0.0150 mL | 0.0750 mL | 0.1501 mL | 0.3752 mL | |
| 100 mM | 0.0120 mL | 0.0600 mL | 0.1201 mL | 0.3002 mL |
BSJ-03-204 Related Classifications
HY-136250 Related Classifications
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