Orelabrutinib |
Catalog No.GC39634
One-Click Copy Product Info
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Orelabrutinib is an orally administered, potent, irreversible and highly selective BTK-inhibitor with an IC50 value of 1.6nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1655504-04-3
Sample solution is provided at 25 µL, 10mM.
Orelabrutinib is an orally administered, potent, irreversible and highly selective BTK-inhibitor with an IC50 value of 1.6nM[1]. Orelabrutinib can reduce the expression of BTK and Mcl-1, and interfere with the activities of the PI3K/AKT signaling pathway and the p38/MAPK signaling pathway[2]. Orelabrutinib has been widely used in mouse models to treat primary immune thrombocytopenia (ITP)[3].
In vitro, Orelabrutinib treatment for 72h significantly inhibited the viability of TMD8 cells, HBL-1 cells and SU-DHL-6 cells with IC50 values of 0.03μM, 0.17μM, and 1.89μM, respectively[4]. Treatment of SU-DHL-4 cells with 60μM Orelabrutinib combined with 2.5μM Chidamide for 48 hours significantly promoted cell apoptosis and induced cell cycle arrest[5]. Treatment with 2μM Orelabrutinib combined with 1μM Selinexor for 48 hours strongly inhibited the NF-κB, P-STAT3 and NFATc1 signaling pathways in OCI-LY10 cells and OCI-LY3 cells[6].
In vivo, Orelabrutinib treatment via oral administration at a dose of 10mg/kg/day for 28 days remarkablely reduced platelet phagocytosis and pro-inflammatory cytokine production in ITP mice[7]. In the TMD8 cell xenograft tumor mouse model, daily oral administration of 10mg/kg dose of Orelabrutinib for 3 weeks significantly inhibited tumor growth[4].
References:
[1] Zhang B, Zhao R, Liang R, et al. Abstract CT132: Orelabrutinib, a potent and selective Bruton's tyrosine kinase inhibitor with superior safety profile and excellent PK/PD properties[J]. Cancer Research, 2020, 80(16_Supplement): CT132-CT132.
[2] Pan G, Zhong M, Yao J, et al. Orelabrutinib and venetoclax synergistically induce cell death in double-hit lymphoma by interfering with the crosstalk between the PI3K/AKT and p38/MAPK signaling[J]. Journal of cancer research and clinical oncology, 2023, 149(9): 5513-5529.
[3] Yu T, Wang L, Ni X, et al. Orelabrutinib, a selective Bruton's tyrosine kinase (BTK) inhibitor in the treatment of primary immune thrombocytopenia (ITP)[J]. Blood, 2021, 138: 3172.
[4] Yu H, Wang X, Li J, et al. Addition of BTK inhibitor orelabrutinib to rituximab improved anti-tumor effects in B cell lymphoma[J]. Molecular Therapy-Oncolytics, 2021, 21: 158-170.
[5] Wu C, Chen S, Wu Z, et al. Chidamide and orelabrutinib synergistically induce cell cycle arrest and apoptosis in diffuse large B-cell lymphoma by regulating the PI3K/AKT/mTOR pathway[J]. Journal of Cancer Research and Clinical Oncology, 2024, 150(2): 98.
[6] Li L, Yang W, Ye R, et al. Combination of Selinexor with BTK Inhibitor for Central Nervous System Diffuse Large B-Cell Lymphoma, Possible Mechanisms and Therapeutic Potential Exploration[J]. Blood, 2023, 142: 3010.
[7] Yu T, Han S, Wang L, et al. Effects of orelabrutinib, a BTK inhibitor, on antibody‐mediated platelet destruction in primary immune thrombocytopenia[J]. British Journal of Haematology, 2025, 206(4): 1186-1199.
| Cell experiment [1]: | |
Cell lines | TMD8 cells |
Preparation Method | TMD8 cells were cultured using RPMI-1640 medium containing 10% fetal bovine serum (FBS), penicillin/streptomycin, glutamine and β-mercaptoethanol, in a humidified environment of a 37°C, 5% CO2 incubator. A 90μl inoculum of cells at a concentration of 5×104/ml was seeded in a 96-well black-bottom plate and incubated with different concentrations of Orelabrutinib (0, 0.1, 1, 2, and 4μM) for 72 hours. The plate was incubated at room temperature on a shaker for 10 minutes, and cell viability was determined using MTT assay. |
Reaction Conditions | 0, 0.1, 1, 2, and 4μM; 72h |
Applications | Orelabrutinib treatment inhibited the proliferation of TMD8 cells in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | Severe combined immunodeficient (SCID) mice |
Preparation Method | The 5×104 splenocytes from immunized CD61-knockout mice against CD61+ platelets were engrafted into CD61+ SCID mice to establish active ITP models, which exhibited profound thrombocytopenia. The ITP mice were divided into the Orelabrutinib group, which was given Orelabrutinib dissolved in 0.5% CMC-Na (10mg/kg) by intragastric administration once daily, and the control group was given 0.5% CMC-Na. The experiment lasted for 28 days, and the platelet counts and inflammatory factors of the mice were analyzed. |
Dosage form | 10mg/kg/day for 28 days; p.o. |
Applications | Orelabrutinib treatment significantly enhanced platelet counts and reduced serum concentrations of IL-6 and IL-1β in ITP mice. |
References: | |
| Cas No. | 1655504-04-3 | SDF | |
| Canonical SMILES | O=C(C1=CC=C(C2CCN(C(C=C)=O)CC2)N=C1C3=CC=C(OC4=CC=CC=C4)C=C3)N | ||
| Formula | C26H25N3O3 | M.Wt | 427.5 |
| Solubility | DMSO: 250 mg/mL (584.80 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3392 mL | 11.6959 mL | 23.3918 mL |
| 5 mM | 467.8 μL | 2.3392 mL | 4.6784 mL |
| 10 mM | 233.9 μL | 1.1696 mL | 2.3392 mL |
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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.
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Quality Control & SDS
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- Purity: >98.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)