BSJ-03-204
Based on 1 Customer Validation
BSJ-03-204 is a PROTAC linking a Cereblon ligand to a CDK ligand, serving as a potent and selective dual degrader of CDK4/6. BSJ-03-204 exhibits IC50 values of 26.9 nM and 10.4 nM against CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 can be utilized for cancer-related research.
(Pink: Cdk4/cyclin D1 and Cdk6/cyclin D2 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
- Purity & Documentation
- References
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Help & FAQs
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All PROTACs Isoforms
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Biological Activity
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CDK4/D1 26.9 nM (IC50) |
CDK6/D1 10.4 nM (IC50) |
BSJ-03-204 (0.0001-100 μM; for 3 or 4 days) has potent anti-proliferative effects on MCL cell lines[1].
BSJ-03-204 (1 μM; for 1 day) potently induces a G1 arrest[1].
BSJ-03-204 (0.1-5 μM; for 4 hours) only resultes in degradation of CDK4/6 in WT cells, not IKZF1/3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCL cell lines (Jeko-1, Mino, Granta-519, Rec-1, and Maver-1 cells)
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Concentration:0.0001-100 μM
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Incubation Time:For 3 or 4 days
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Result:Had potent anti-proliferative effects on mantle cell lymphoma (MCL) cell lines.
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Cell Line:Granta-519 cells
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Concentration:1 μM
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Incubation Time:For 1 day
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Result:Potently induced a G1 arrest.
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Cell Line:Wildtype (WT) or Crbn-/- Jurkat cells
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Concentration:0.1, 0.5, 1, 5 μM
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Incubation Time:For 4 hours
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Result:Only resulted in degradation of CDK4/6 in WT cells, not IKZF1/3.
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
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)
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.
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.
Purity & Documentation
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Data Sheet (272 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 |
|---|---|---|---|---|---|
| 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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