BSJ-05-037 |
Catalog No.GC81298
One-Click Copy Product Info
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BSJ-05-037 is an ITK PROTAC degrader that effectively targets and degrades ITK in T-cell lymphoma cell lines.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2756388-01-7
Sample solution is provided at 25 µL, 10mM.
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In Vivo, BSJ-05-037 (50 mg/kg; i.p.; every 8 hours; 3 total doses/once every other day; 14 days) induces ITK degradation, reduces GATA-3 expression, inhibits PLCγ1, decreases tumor volume, and reverses chemoresistance in Hut78/H9 cutaneous T-cell lymphoma xenografts in mice[1].
In Vitro, BSJ-05-037 (0.001-10 μM; 2-16 h) potently induces time- and concentration-dependent degradation of ITK in DERL-2 and Hut78 cells, and this degradation is CRBN-dependent[1]. BSJ-05-037 (1 μM; 10 days) potently inhibits the proliferation of DERL-2 and Jurkat T-cell lymphoma cells[1]. BSJ-05-037 (0.025-0.5 μM; 8 h) dose-dependently inhibits the phosphorylation of PLCγ1 in DERL-2 cells[1]. BSJ-05-037 (1 μM; 24 h-3 days) blocks TCR-induced upregulation of GATA-3 and restores the sensitivity of T8ML-1 cells to Vincristine, thereby overcoming drug resistance mediated by the ITK/NF-κB/GATA-3 axis[1]. BSJ-05-037 (1 μM; 24 h-4 days) induces nearly complete ITK degradation and reduces GATA-3 levels by over 90% in Hut78 and H9 cutaneous T-cell lymphoma cells, while also enhancing the sensitivity of these cells to Vincristine during the 4-day treatment[1].
References:
[1]. Jiang B, et al. ITK degradation to block T cell receptor signaling and overcome therapeutic resistance in T cell lymphomas. Cell Chem Biol. 2023;30(4):383-393.e6.
[2]. Tigu AB, et al. Proteolysis targeting chimeric-based technology in myeloma and lymphoma. Mol Cancer Ther. Published online January 2, 2026.
[3]. Miletić N, et al. Workflow for E3 Ligase Ligand Validation for PROTAC Development. ACS Chem Biol. 2025;20(2):507-521.
| Cas No. | 2756388-01-7 | SDF | |
| Formula | C51H59N9O10S2 | M.Wt | 1022.2 |
| Solubility | DMSO: 100 mg/mL (97.83 mM; Need ultrasonic) | Storage | Store at 4°C, away from moisture and light |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 978.3 μL | 4.8914 mL | 9.7828 mL |
| 5 mM | 195.7 μL | 978.3 μL | 1.9566 mL |
| 10 mM | 97.8 μL | 489.1 μL | 978.3 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)