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Formula | C25H24N6O2 |
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Molecular Weight | 440.5 | CAS No. | 936563-96-1 | |
Solubility (25°C)* | In vitro | DMSO | 88 mg/mL (199.77 mM) | |
Ethanol | 3 mg/mL (6.81 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Ibrutinib is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc. Ibrutinib is applicable as a Btk ligand in the synthesis of a series of PROTACs including P13I. | |||||||||||
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Targets |
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In vitro | Ibrutinib shows the potent and irreversible inhibitory effect and selectivity for Btk enzymatic activity. In BCR pathway-activated DOHH2 cell line, Ibrutinib inhibits autophosphorylation of Btk, phosphorylation of Btk's physiological substrate PLCγ, and phosphorylation of further downstream kinase, ERK with IC50 of 11 nM, 29 nM and 13 nM, respectively. [1] Ibrutinib exhibits a significant dose-dependent and time-dependent induction of cytotoxicity in chronic lymphocytic leukemia (CLL) cells. In addition, Ibrutinib induces cell death depending on caspase pathway activation and antagonizes the ability of CLL cells to proliferate after TLR signaling. [2] A recent study shows that Ibrutinib inhibits BCR-activated primary B cell proliferation with IC50 of 8 nM and results in inhibition of TNFα, IL-1β and IL-6 production in primary monocytes with IC50 of 2.6 nM, 0.5 nM and 3.9 nM, respectively. [3] |
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In vivo | In a collagen-induced arthritis model, Ibrutinib significantly reduces clinical arthritis scores reflecting paw swelling and joint inflammation by inhibiting B-cell activation. In a MRL-Fas(lpr) lupus model, Ibrutinib reduces renal disease and autoantibody production. [1] In an adoptive transfer TCL1 mouse model of CLL, Ibrutinib (25 mg/kg/day) causes a transient early lymphocytosis, and delays CLL disease progression. [4] |
Kinase Assay: |
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Data from [Data independently produced by J Cell Sci, 2015, 128(2), 251-65]
Data from [Data independently produced by J Biol Chem, 2015, 290(18), 11557-68]
Data from [Data independently produced by Blood Cancer J, 2014, 4, e181]
Data from [Data independently produced by Br J Haematol, 2014, 166(6), 849-61]
Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3] | PubMed: 38262581 |
T-bet+ B cells are activated by and control endogenous retroviruses through TLR-dependent mechanisms [ Nat Commun, 2024, 15(1):1229] | PubMed: 38336876 |
T-bet+ B cells are activated by and control endogenous retroviruses through TLR-dependent mechanisms [ Nat Commun, 2024, 15(1):1229] | PubMed: 38336876 |
Immunotherapy-resistant acute lymphoblastic leukemia cells exhibit reduced CD19 and CD22 expression and BTK pathway dependency [ J Clin Invest, 2024, 134(8)e175199] | PubMed: 38376944 |
Dialog between mantle cell lymphoma cells and lymphoma-associated macrophages underlies ibrutinib resistance [ J Adv Res, 2024, S2090-1232(24)00366-7] | PubMed: 39168245 |
Impact of therapeutic inhibition of oncogenic cell signaling tyrosine kinase on cell metabolism: in vivo-detectable metabolic biomarkers of inhibition [ J Transl Med, 2024, 22(1):622] | PubMed: 38965536 |
EFNB1 levels determine distinct drug response patterns guiding precision therapy for B-cell neoplasms [ iScience, 2024, 27(1):108667] | PubMed: 38155773 |
Ibrutinib-induced pulmonary angiotensin-converting enzyme activation promotes atrial fibrillation in rats [ iScience, 2024, 27(2):108926] | PubMed: 38357670 |
CAD204520 Targets NOTCH1 PEST Domain Mutations in Lymphoproliferative Disorders [ Int J Mol Sci, 2024, 25(2)766] | PubMed: 38255842 |
Impact of ibrutinib on inflammation in a mouse model of Graves' orbitopathy [ Front Endocrinol (Lausanne), 2024, 15:1420024] | PubMed: 39280007 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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