| ln Vitro |
BSJ-05-037 (0.001-10 μM; 2-16 h) effectively induced the degradation of ITK in DEL-2 and Hut78 cells in a time- and concentration-dependent manner, and was dependent on CRBN[1]. BSJ-05-037 (1 μM; 10 d) effectively inhibited the proliferation of DEL-2 and Jurkat T-cell lymphoma cells[1]. BSJ-05-037 (0.025-0.5 μM; 8 d) dose-dependently inhibited the phosphorylation of PLCγ1 in DEL-2 cells[1]. BSJ-05-037 (1 μM; 24 d to 3 d) blocked TCR-induced upregulation of GATA-3 and restored the sensitivity of T8ML-1 cells to vincristine(A), thereby overcoming drug resistance mediated by the ITK/NF-κB/GATA-3 axis[1]. BSJ-05-037 (1 μM; 24 hours to 4 days) induced almost complete degradation of ITK in Hut78 and H9 cutaneous T-cell lymphoma cells and reduced GATA-3 levels by more than 90%, while enhancing the sensitivity of these cells to vincristine during the 4-day treatment period [1].
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| ln Vivo |
BSJ-05-037 (50 mg/kg; intraperitoneal injection; every 8 hours; 3 times every other day; 14 days) can induce ITK degradation, reduce GATA-3 expression, inhibit PLCγ1, reduce tumor volume, and reverse chemotherapy resistance in xenografts of mouse Hut78/H9 cutaneous T-cell lymphoma [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: DERL-2, Hut78 cells Tested Concentrations: 0.001, 0.01, 0.1, 1, 10 μM Incubation Duration: 2, 4, 8, 16 hours Experimental Experimental Results: After 16 hours of treatment, ITK protein was induced to undergo potent degradation in a dose-dependent manner (IC50 = 17.6~41.8 nM). Cell viability assay [1] Cell Types: T-cell lymphoma cell lines (DERL-2, Jurkat) Tested Concentrations: 1 μM Incubation Duration: 10 days Experimental Results: After 10 days, the viability of DERL-2 cells decreased to less than 10% of that of the DMSO control group. This induced growth inhibition of Jurkat cells. Western Blot analysis [1] Cell Types: DERL-2 cells Tested Concentrations: 0.025, 0.1, 0.25, 0.5 μM Incubation Duration: 8 hours Experimental Results: It resulted in dose-dependent inhibition of PLCγ1 phosphorylation.
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| Animal Protocol |
Animal/Disease Models:NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ (NSG) mice (9-10 weeks old) [1]
Doses: 50 mg/kg Route of Administration: Intraperitoneal injection; every 8 hours; 3 times/every other day; for 14 days Experimental Results: Induced 99.2% ITK degradation in xenograft tumors. GATA-3 protein levels in tumors decreased by more than 90% after treatment. With monotherapy, the average tumor volume shrank to approximately 1100 mm3 on day 14. When combined with vincristine, tumor growth almost completely stopped, and the average tumor volume shrank to approximately 150 mm3 on day 14. NF-κB pathway gene enrichment. Downregulation of GATA3, IL2, CD69, and NF-κB regulator NFKBIA leads to enrichment of other TCR pathway signatures, including inflammatory responses, STAT3 and STAT5 signaling pathways, MYC targets, and cell cycle regulation. |
| References |
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| CAS # |
2756388-01-7
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| Appearance |
White to light yellow solid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: 请将本产品存放在密封且受保护的环境中（例如氮气下），避免暴露在潮湿和光照下。 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~97.83 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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