Btk inhibitor 1 - CAS 1412418-47-3
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Not Intended for Therapeutic Use. For research use only.
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Btk inhibitor 1 is a pyrazolo[3,4-d]pyrimidine derivative as a Btk kinase inhibitor.
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Btk inhibitor 1
1.Bruton's tyrosine kinase inhibitor restrains Wnt signaling in chronic lymphocytic leukemia.
Li PP1, Lu K1, Geng LY1, Zhou XX1, Li XY1, Wang X1. Mol Med Rep. 2016 Apr 12. doi: 10.3892/mmr.2016.5111. [Epub ahead of print]
The B-cell receptor (BCR) signaling pathway serves an important role in the pathogenesis of chronic lymphocytic leukemia (CLL), and has been identified as a novel and effective therapeutic target of CLL, with particular focus its kinase factor, BTK. Previous studies have focused on combining the BTK inhibitor with additional chemotherapeutic agents to improve the prognosis of patients with CLL. Further investigation into the mechanism of the BTK inhibitor would promote an understanding of the pathogenesis of CLL. The current study investigated the association between ibrutinib and the Wnt signaling pathway, additionally focussing upon one of its regulators, metadherin (MTDH), which has been identified to be overexpressed in CLL and is considered a promoter of the Wnt pathway. The experiments in the current study were performed in the MEC-1 CLL cell line. Results indicated that MTDH, β-catenin and lymphoid-enhancing factor-1 were inhibited subsequent to ibrutinib treatment.
2.BCR signaling inhibitors differ in their ability to overcome Mcl-1-mediated resistance of CLL B cells to ABT-199.
Bojarczuk K1, Sasi BK1, Gobessi S1, Innocenti I2, Pozzato G3, Laurenti L2, Efremov DG4. Blood. 2016 Apr 19. pii: blood-2015-10-675009. [Epub ahead of print]
The Bcl-2 antagonist ABT-199 has demonstrated promising clinical activity in patients with CLL. ABT-199 is strongly cytotoxic against unstimulated peripheral blood CLL cellsin vitro, but is much less effective against CLL cells that have received survival signals from the microenvironment. In particular, stimulation of CLL cells with CD40L results in substantial resistance that is mediated by induction of the antiapoptotic Bcl-2 family proteins Bcl-xLand Bfl-1. In the present study we investigated whether resistance to ABT-199 can be conferred by B-cell receptor (BCR) stimulation, which is another important survival signal from the leukemic microenvironment. We show that sustained BCR stimulation results in significant ABT-199-resistance, which correlates with induction of the antiapoptotic protein Mcl-1 and less consistently with downregulation of proapoptotic Bmf, Hrk and BimEL A major role for Mcl-1 in conferring ABT-199 resistance is additionally supported by knockdown and enforced expression experiments with primary CLL cells.
3.The Addition of the BTK Inhibitor Ibrutinib to Anti-CD19 Chimeric Antigen Receptor T Cells (CART19) Improves Responses against Mantle Cell Lymphoma.
Ruella M1, Kenderian SS2, Shestova O1, Fraietta JA1, Qayyum S3, Zhang Q3, Maus MV4, Liu X3, Nunez-Cruz S1, Klichinsky M1, Kawalekar OU1, Milone M5, Lacey SF6, Mato A7, Schuster SJ7, Kalos M6, June CH5, Gill S8, Wasik MA9. Clin Cancer Res. 2016 Jan 27. [Epub ahead of print]
PURPOSE: Responses to therapy with chimeric antigen receptor T cells recognizing CD19 (CART19, CTL019) may vary by histology. Mantle cell lymphoma (MCL) represents a B-cell malignancy that remains incurable despite novel therapies such as the BTK inhibitor ibrutinib, and where data from CTL019 therapy are scant. Using MCL as a model, we sought to build upon the outcomes from CTL019 and from ibrutinib therapy by combining these in a rational manner.
4.Btk Inhibitor RN983 Delivered by Dry Powder Nose-only Aerosol Inhalation Inhibits Bronchoconstriction and Pulmonary Inflammation in the Ovalbumin Allergic Mouse Model of Asthma.
Phillips JE1, Renteria L1, Burns L1, Harris P1, Peng R1, Bauer CM1, Laine D1, Stevenson CS1. J Aerosol Med Pulm Drug Deliv. 2016 Apr 25. [Epub ahead of print]
BACKGROUND: In allergen-induced asthma, activated mast cells start the lung inflammatory process with degranulation, cytokine synthesis, and mediator release. Bruton's tyrosine kinase (Btk) activity is required for the mast cell activation during IgE-mediated secretion.
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CAS 1412418-47-3 Btk inhibitor 1

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