別品名 |
Ibrutinib
|
別包装 |
あり
|
純度 |
>=99%
|
分子量 |
440.5
|
CAS RN® |
936563-96-1
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化合物の概要 |
BTK and IL-2-inducible kinase inhibitor.
|
構造 |
C25H24N6O2
|
溶媒 |
DMSO88 mg/mL (199.77 mM)Ethanol45 mg/mL (102.15 mM)WaterInsoluble
|
使用目的 |
PCI-32765 is an irreversible inhibitor of Bruton’s tyrosine kinase (BTK), an enzyme that plays a significant role in B-cell receptor signaling and B-cell malignancies and autoimmune diseases such as x-linked agammaglobulinemia, chronic lymphocytic leukemia, and non-Hodgkin’s lymphoma. This compound displays anticancer chemotherapeutic, anti-metastatic, immunomodulatory, and anti-fibrotic activities. PCI-32765’s inhibition of BTK prevents IgE-mediated activation of basophils, inhibits signaling from macrophages and mast cells, and inhibits cell migration and survival in cellular and animal models of chronic lymphocytic leukemia. Additionally, PCI-32765 inhibits IL-2-inducible kinase and suppresses the development of fibrosis in pancreatic adenocarcinoma models.
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その他 |
[融点]158.3 oC
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参考文献 |
Masso-Valles D, Jauset T, Serrano E, et al. Ibrutinib exerts potent antifibrotic and antitumor activities in mouse models of pancreatic adenocarcinoma. Cancer Res. 2015 Apr 15;75(8):1675-81. PMID: 25878147.Dubovsky JA, Beckwith KA, Natarajan G, et al. Ibrutinib is an irreversible molecular inhibitor of ITK driving a Th1 selective pressure in T-lymphocytes. Blood. 2013 Jul 25. [Epub ahead of print]. PMID: 23886836.Ponader S, Chen SS, Buggy JJ, et al. The Bruton tyrosine kinase inhibitor PCI-32765 thwarts chronic lymphocytic leukemia cell survival and tissue homing in vitro and in vivo. Blood. 2012 Feb 2;119(5):1182-9. PMID: 22180443.Chang BY, Huang MM, Francesco M, et al. The Bruton tyrosine kinase inhibitor PCI-32765 ameliorates autoimmune arthritis by inhibition of multiple effector cells. Arthritis Res Ther. 2011 Jul 13;13(4):R115. PMID: 21752263.MacGlashan D Jr, Honigberg LA, Smith A, et al. Inhibition of IgE-mediated secretion from human basophils with a highly selective Bruton's tyrosine kinase, Btk, inhibitor. Int Immunopharmacol. 2011 Apr;11(4):475-9. PMID: 21238622.Honigberg LA, Smith AM, Sirisawad M, et al. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80. PMID: 20615965.
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メーカー |
品番 |
包装 |
LKT
|
P0932
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5 MG
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※表示価格について
当社在庫 |
なし
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納期目安 |
1週間程度
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保存温度 |
常温
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