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10mg |
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25mg |
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100mg |
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Purity: ≥98%
Orelabrutinib (ICP-022; ICP022; ICP 022) is an oral bioavailable, new generation and irreversible/covalent Bruton's tyrosine kinase (BTK) inhibitor with the potential to be used for the treatment of cancer such as B-cell lymphomas and autoimmune indications. Orelabrutinib was first approved in China in December 2020 for the treatment of patients who have had at least one prior treatment for mantle cell lymphoma (MCL), chronic lymphocytic leukemia (CLL), or small lymphocytic lymphoma (SLL). China and the United States are conducting clinical trials for a variety of orelabrutinib indications.
Targets |
BTK
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ln Vitro |
Orelabrutinib has an IC50 value of 1.6 nM and effectively suppresses BTK enzymatic activity. Orelabrutinib only targets BTK with > 90% inhibition in a parallel KINOMEscan assay at 1 μM against a panel of 456 kinases, whereas ibrutinib inhibits many other kinases, such as EGFR, TEC, and BMX, indicating orelabrutinib's superior kinase selectivity.[2]
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ln Vivo |
Orelabrutinib exhibits a good PK profile in preclinical PK/PD studies, with an ideal T1/2 of ~1.5–4 h, good oral bioavailability of ~20–80%, and prolonged BTK target occupancy. In the GLP toxicological investigations in rats and dogs, the higher selectivity results in an enhanced safety profile and a wide safety window.[2]
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References |
Molecular Formula |
C₂₆H₂₅N₃O₃
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Molecular Weight |
427.50
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Exact Mass |
427.19
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Elemental Analysis |
C, 73.05; H, 5.89; N, 9.83; O, 11.23
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CAS # |
1655504-04-3
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Related CAS # |
1655504-04-3
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Appearance |
Solid powder
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SMILES |
C=CC(=O)N1CCC(CC1)C2=NC(=C(C=C2)C(=O)N)C3=CC=C(C=C3)OC4=CC=CC=C4
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InChi Key |
MZPVEMOYADUARK-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C26H25N3O3/c1-2-24(30)29-16-14-18(15-17-29)23-13-12-22(26(27)31)25(28-23)19-8-10-21(11-9-19)32-20-6-4-3-5-7-20/h2-13,18H,1,14-17H2,(H2,27,31)
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Chemical Name |
2-(4-phenoxyphenyl)-6-(1-prop-2-enoylpiperidin-4-yl)pyridine-3-carboxamide
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Synonyms |
ICP022; Orelabrutinib; ICP-022; ICP 022
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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 |
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: 86~100 mg/mL (201.2~233.9 mM)
Ethanol: ~10 mg/mL (~23.4 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.85 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3392 mL | 11.6959 mL | 23.3918 mL | |
5 mM | 0.4678 mL | 2.3392 mL | 4.6784 mL | |
10 mM | 0.2339 mL | 1.1696 mL | 2.3392 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05036577 | Active Recruiting |
Drug: Orelabrutinib Drug: Rituximab |
Primary Central Nervous System Lymphoma |
Huashan Hospital | October 10, 2021 | Phase 1 |
NCT04711148 | Active Recruiting |
Other: placebo Drug: orelabrutinib |
Relapsing Remitting Multiple Sclerosis |
Beijing InnoCare Pharma Tech Co., Ltd. |
March 1, 2021 | Phase 2 |
NCT06115824 | Active Recruiting |
Drug: Orelabrutinib | Primary Central Nervous System Lymphoma |
Huashan Hospital | August 10, 2023 | |
NCT04304040 | Active Recruiting |
Drug: Orelabrutinib Drug: Recombinant humanized monoclonal antibody MIL62 injection |
B-cell Lymphoma Recurrent B-cell Lymphoma Refractory |
Beijing InnoCare Pharma Tech Co., Ltd. |
July 28, 2020 | Phase 1 Phase 2 |
NCT04014205 | Active Recruiting |
Drug: Orelabrutinib (ICP-022) |
Part 1:r/r B-cell Malignancies Part 2:B-cell Malignancies |
Beijing InnoCare Pharma Tech Co., Ltd. |
November 18, 2019 | Phase 1 Phase 2 |