BLK degrader 1
Based on 1 Customer Validation
BLK degrader 1 is a selective B lymphoid tyrosine kinase (BLK) degrader with a BLK DC50 of 49 nM in cells. BLK degrader 1 induces ubiquitin-proteasome-dependent BLK degradation through binding. BLK degrader 1 exhibits anticancer activity in multiple B lymphocyte cell lines and downregulates CDK2 protein levels. BLK degrader 1 can be used in research related to B cell lymphoma.
For research use only. We do not sell to patients.
- Purity : 98.94%
- CAS No.: 3049215-64-4
- Formula: C32H25F3N6O2
- Molecular Weight:582.58
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
Biological Activity
Description
IC50 & Target
[1]|
Blk 49 nM (DC50) |
Blk 443 nM (IC50) |
CDK2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DOHH-2 | GI50 |
0.13 μM
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Antiproliferative activity against human DoHH2 cells assessed as inhibition of cell growth.
Antiproliferative activity against human DoHH2 cells assessed as inhibition of cell growth.
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37163946 |
| SU-DHL-4 | GI50 |
0.18 μM
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Antiproliferative activity against human SU-DHL-4 cells assessed as inhibition of cell growth.
Antiproliferative activity against human SU-DHL-4 cells assessed as inhibition of cell growth.
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37163946 |
| SU-DHL-6 | GI50 |
0.36 μM
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Antiproliferative activity against human SU-DHL-6 cells assessed as inhibition of cell growth.
Antiproliferative activity against human SU-DHL-6 cells assessed as inhibition of cell growth.
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37163946 |
| DOHH-2 | DC50 |
0.095 μM
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Degradation of BLK in human DoHH2 cells by Western blot analysis.
Degradation of BLK in human DoHH2 cells by Western blot analysis.
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37163946 |
| SU-DHL-4 | DC50 |
0.27 μM
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Degradation of BLK in human SU-DHL-4 cells by Western blot analysis.
Degradation of BLK in human SU-DHL-4 cells by Western blot analysis.
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37163946 |
| SU-DHL-6 | DC50 |
0.23 μM
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Degradation of BLK in human SU-DHL-6 cells by Western blot analysis.
Degradation of BLK in human SU-DHL-6 cells by Western blot analysis.
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37163946 |
In Vitro
BLK degrader 1 (Compound 9) (3-3000 nM; 12 h) effectively degrades BLK in Ramos cells with a DC50 of 49 nM[1].
BLK degrader 1 inhibits recombinant BLK and BTK kinases, with an IC50 of 443 nM for BLK[1].
BLK degrader 1 (0.01-3 μM; 12 h) selectively degrades BLK in Ramos and Jurkat cells without significantly interfering with other SRC and TEC family kinases[1].
BLK degrader 1 (1 μM; 6 h) induces time-dependent BLK degradation in Ramos cells[1].
BLK degrader 1 (0.1-0.3 μM; 72 h) selectively inhibits the proliferation of B lymphoid cell lines[1].
BLK degrader 1 effectively inhibits the growth of DoHH2, SU-DHL-4, and SU-DHL-6 cells, which may primarily result from BLK degradation[1].
BLK degrader 1 (0.1-1 μM; 48 h) reduces CDK2 protein levels in DoHH2 and SU-DHL-6 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:Ramos cells
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Concentration:3, 10, 30, 100, 300 and 3000 nM
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Incubation Time:12 h
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Result:Effectively degraded BLK with a DC50 of 49 nM and a Dmax of 97%.
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Cell Line:Ramos and Jurkat cells
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Concentration:0.01, 0.1 and 1 μM (Ramos cells); 0.1, 0.3, 1 and 3 μM (Jurkat cells)
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Incubation Time:12 h
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Result:Demonstrated a high level of degradation selectivity for BLK over other kinases.
Although it could partially degrade LCK in Jurkat cells, it was less effective, with Dmax values < 50%, and required higher concentrations.
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Cell Line:Ramos cells
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Concentration:1 μM
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Incubation Time:6 h
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Result:BLK degradation was observed at 3 h after treatment, and maximum degradation was achieved at 6 h.
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Cell Line:DoHH2 and SU-DHL-6 cells
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Concentration:0.1, 0.3 and 1 μM
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Incubation Time:48 h
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Result:At 1 μM for 48 h, significantly reduced CDK2 protein levels in DoHH2 and SU-DHL-6 cells.
Chemical Information
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CAS No. 3049215-64-4
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Appearance Solid
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Molecular Weight 582.58
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Formula C32H25F3N6O2
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Color Off-white to light yellow
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SMILES
CC1=CC=C(C=C1C(NC2=CN=C(N=C2)NC3=CC=CC(N)=C3)=O)NC(C4=CC=C(C=C4)C5=CC(C(F)(F)F)=CC=C5)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (171.65 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)
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 (4.29 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.
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.
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 (273 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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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. 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 | 1.7165 mL | 8.5825 mL | 17.1650 mL | 42.9126 mL |
| 5 mM | 0.3433 mL | 1.7165 mL | 3.4330 mL | 8.5825 mL | |
| 10 mM | 0.1717 mL | 0.8583 mL | 1.7165 mL | 4.2913 mL | |
| 15 mM | 0.1144 mL | 0.5722 mL | 1.1443 mL | 2.8608 mL | |
| 20 mM | 0.0858 mL | 0.4291 mL | 0.8583 mL | 2.1456 mL | |
| 25 mM | 0.0687 mL | 0.3433 mL | 0.6866 mL | 1.7165 mL | |
| 30 mM | 0.0572 mL | 0.2861 mL | 0.5722 mL | 1.4304 mL | |
| 40 mM | 0.0429 mL | 0.2146 mL | 0.4291 mL | 1.0728 mL | |
| 50 mM | 0.0343 mL | 0.1717 mL | 0.3433 mL | 0.8583 mL | |
| 60 mM | 0.0286 mL | 0.1430 mL | 0.2861 mL | 0.7152 mL | |
| 80 mM | 0.0215 mL | 0.1073 mL | 0.2146 mL | 0.5364 mL | |
| 100 mM | 0.0172 mL | 0.0858 mL | 0.1717 mL | 0.4291 mL |
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