BSJ-05-037
Based on 1 Customer Validation
BSJ-05-037 is an ITK PROTAC degrader that effectively targets and degrades ITK in T-cell lymphoma cell lines. BSJ-05-037 blocks the activation of the NF-κB/GATA-3 signaling pathway, inhibits PLCγ1 phosphorylation, and reduces the proliferative capacity of T-cell lymphoma cells. BSJ-05-037 enhances the sensitivity of T-cell lymphoma cells to chemotherapy. In mouse models of T-cell lymphoma, BSJ-05-037 induces ITK degradation, reduces GATA-3 expression, decreases tumor volume, and reverses chemotherapy resistance. BSJ-05-037 is applicable to research related to T-cell lymphoma.
(Pink: Itk ligand (HY-11092); Blue: Cereblon ligand (HY-103597); Black: linker (HY-W036393)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.83%
- CAS 番号: 2756388-01-7
- 分子式: C51H59N9O10S2
- 分子量:1022.20
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and 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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
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Cereblon |
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 (HY-N0488A), 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DERL-2、Hut78 cells
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Concentration:0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:2, 4, 8, 16 h
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Result:Induced potent degradation of ITK protein in a dose-dependent manner after a 16 h treatment (IC50 = 17.6~ 41.8 nM).
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Cell Line:T-cell lymphoma cell lines (DERL-2, Jurkat)
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Concentration:1 μM
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Incubation Time:10 days
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Result:Reduced DERL-2 cell viability to <10% of DMSO control after 10 days.
Induced growth inhibition in Jurkat cells.
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Cell Line:DERL-2 cells
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Concentration:0.025, 0.1, 0.25, 0.5 μM
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Incubation Time:8 h
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Result:Resulted in dose-dependent inhibition of PLCγ1 phosphorylation.
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Cell Line:T8ML1 cells
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Concentration:1 μM
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Incubation Time:24 h
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Result:Induced potent ITK degradation and abrogated TCR-dependent upregulation of GATA-3.
| Species | Dose | Route | T1/2 | Cmax |
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| Mice[1] | 10 mg/kg | i.p. | 1.9 h | 3.4 μM |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ (NSG) mice (9-10 weeks old)[1]
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Dosage:50 mg/kg
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Administration:i.p.; every 8 hours; 3 total doses/ once every other day; 14 days
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Result:Induced 99.2% degradation of ITK in xenografted tumors.
Reduced GATA-3 protein levels by >90% in treated tumors.
Reduced mean tumor volume to ~1100 mm3 by day 14 as monotherapy.
Achieved almost complete tumor stasis, with mean tumor volume reduced to ~150 mm3 by day 14 when combined with vincristine.
Enriched NF-κB pathway gene.
Downregulated GATA3, IL2, CD69, and the NF-κB regulators NFKBIA.
Resulted in an enrichment of signatures for other TCR pathways including inflammatory response,
STAT3 and STAT5 signaling, MYC targets and cell cycle regulation.
化学情報
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CAS 番号 2756388-01-7
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性状 Solid
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分子量 1022.20
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分子式 C51H59N9O10S2
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Color White to light yellow
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SMILES
O=C(NC1=NC=C(SC2=CC(C(N3CCN(C(C)=O)CC3)=O)=C(OC)C=C2C)S1)C4=CC=C(N5CCN(CCCCCCCNC(COC6=C7C(C(N(C8CCC(NC8=O)=O)C7=O)=O)=CC=C6)=O)CC5)C=C4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
DMSO : 100 mg/mL (97.83 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 (sealed storage, away from moisture and 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (sealed storage, away from moisture and 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.
純度とドキュメンテーション
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データシート (277 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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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[2]. Tigu AB, et al. Proteolysis targeting chimeric-based technology in myeloma and lymphoma. Mol Cancer Ther. Published online January 2, 2026. [Content Brief]
[3]. Miletić N, et al. Workflow for E3 Ligase Ligand Validation for PROTAC Development. ACS Chem Biol. 2025;20(2):507-521. [Content Brief]
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 (sealed storage, away from moisture and 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 | 0.9783 mL | 4.8914 mL | 9.7828 mL | 24.4571 mL |
| 5 mM | 0.1957 mL | 0.9783 mL | 1.9566 mL | 4.8914 mL | |
| 10 mM | 0.0978 mL | 0.4891 mL | 0.9783 mL | 2.4457 mL | |
| 15 mM | 0.0652 mL | 0.3261 mL | 0.6522 mL | 1.6305 mL | |
| 20 mM | 0.0489 mL | 0.2446 mL | 0.4891 mL | 1.2229 mL | |
| 25 mM | 0.0391 mL | 0.1957 mL | 0.3913 mL | 0.9783 mL | |
| 30 mM | 0.0326 mL | 0.1630 mL | 0.3261 mL | 0.8152 mL | |
| 40 mM | 0.0245 mL | 0.1223 mL | 0.2446 mL | 0.6114 mL | |
| 50 mM | 0.0196 mL | 0.0978 mL | 0.1957 mL | 0.4891 mL | |
| 60 mM | 0.0163 mL | 0.0815 mL | 0.1630 mL | 0.4076 mL | |
| 80 mM | 0.0122 mL | 0.0611 mL | 0.1223 mL | 0.3057 mL |
BSJ-05-037 関連分類
HY-185206 関連分類
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