BSJ-01-175
Based on 1 Customer Validation
BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.88%
- CAS No.: 2227392-55-2
- Formule: C30H33ClN6O2
- Masse moléculaire:545.08
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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CDK12 |
CDK13 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Kelly | IC50 |
225.3 nM
Compound: 22a; BSJ-01-175
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Antiproliferative activity against human Kelly cells harboring CDK12 C1039F mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human Kelly cells harboring CDK12 C1039F mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
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[PMID: 33945934] |
| Kelly | IC50 |
42.2 nM
Compound: 22a; BSJ-01-175
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Antiproliferative activity against human Kelly cells harboring wild type CDK12 assessed as reduction in cell viability incubated for 72 hrs by CelTiter-Glo assay
Antiproliferative activity against human Kelly cells harboring wild type CDK12 assessed as reduction in cell viability incubated for 72 hrs by CelTiter-Glo assay
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[PMID: 33945934] |
BSJ-01–175 (0-10 μM; 72 hours) causes a 5-fold increase in cell viability compared to the wild type (WT), indicating strong dependence on covalent bond formation with Cys1039[1].
BSJ-01–175 (0-10 μM; 72 hours) slightly decreases the activity of TC71 Ewing sarcoma cells compared to THZ531[1].
BSJ-01–175 (0-5 μM) specifically targets CDK12/13 and suppresses the transcription of BRAC1 and BRAC2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Kelly wild type or CDK12C1039F cells
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Concentration:0-10 μM
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Incubation Time:72 hours
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Result:Observed a 5-fold increase in cell viability compared to the wild type (WT), indicating strong dependence on covalent bond formation with Cys1039.
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Cell Line:TC71 Ewing sarcoma cells
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Concentration:0-10 μM
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Incubation Time:72 hours
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Result:Slightly decreased the activity compared to THZ531.
Assessment of Pharmacokinetics (PK) profile of BSJ-01-175 in mouse[1].
| Route | Dose (mg/kg) | Tmax (h) | Cmax (ng/mL) | AUClast (h•ng/mL) | T1/2 (h) | CL (mL/min/kg) | VSS (L/kg) | F (%) |
| IV | 3 | 1511 | 1832 | 2.2 | 24.9 | 3.9 | ||
| PO | 10 | 2 | 272 | 1043 | 17 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice (BALB/c, 7-8 weeks) bearing TC71 Ewing sarcoma cells[1]
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Dosage:10 mg/kg
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Administration:i.p.; daily for 3 weeks
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Result:Led to a significant suppression of tumor growth throughout 3 weeks of drug treatment period.
Chemical Information
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CAS No. 2227392-55-2
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Appearance Solid
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Masse moléculaire 545.08
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Formule C30H33ClN6O2
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Color White to off-white
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SMILES
ClC1=CN=C(N[C@H]2C[C@@H](CCC2)OC3=CC=C(C=C3)NC(/C=C/CN(C)C)=O)N=C1C4=CNC5=CC=CC=C45
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (183.46 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. 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. 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.59 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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.
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.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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. 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 | 1.8346 mL | 9.1730 mL | 18.3459 mL | 45.8648 mL |
| 5 mM | 0.3669 mL | 1.8346 mL | 3.6692 mL | 9.1730 mL | |
| 10 mM | 0.1835 mL | 0.9173 mL | 1.8346 mL | 4.5865 mL | |
| 15 mM | 0.1223 mL | 0.6115 mL | 1.2231 mL | 3.0577 mL | |
| 20 mM | 0.0917 mL | 0.4586 mL | 0.9173 mL | 2.2932 mL | |
| 25 mM | 0.0734 mL | 0.3669 mL | 0.7338 mL | 1.8346 mL | |
| 30 mM | 0.0612 mL | 0.3058 mL | 0.6115 mL | 1.5288 mL | |
| 40 mM | 0.0459 mL | 0.2293 mL | 0.4586 mL | 1.1466 mL | |
| 50 mM | 0.0367 mL | 0.1835 mL | 0.3669 mL | 0.9173 mL | |
| 60 mM | 0.0306 mL | 0.1529 mL | 0.3058 mL | 0.7644 mL | |
| 80 mM | 0.0229 mL | 0.1147 mL | 0.2293 mL | 0.5733 mL | |
| 100 mM | 0.0183 mL | 0.0917 mL | 0.1835 mL | 0.4586 mL |
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