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イブルチニブ

 イブルチニブ 化学構造式
936563-96-1
CAS番号.
936563-96-1
化学名:
イブルチニブ
别名:
イブルチニブ;イブルチニブ;イブルチニブ (JAN)
英語化学名:
Ibrutinib
英語别名:
CS-188;PCI-32765;IBRUTINIB;Lbrutinib;Ibrutinib (API);Ibrutinib, >=98%;Ibrutinib fandachem;According to lu for;PCI-32765 (Ibrutinib);Ibrutinib (PCI-32765)
CBNumber:
CB12515873
化学式:
C25H24N6O2
分子量:
440.5
MOL File:
936563-96-1.mol

イブルチニブ 物理性質

沸点 :
715.0±60.0 °C(Predicted)
比重(密度) :
1.34
酸解離定数(Pka):
4.09±0.30(Predicted)
CAS データベース:
936563-96-1

安全性情報

有毒物質データの 936563-96-1(Hazardous Substances Data)

イブルチニブ 価格

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入

イブルチニブ 化学特性,用途語,生産方法

用途

イブルチニブ(Ibrutinib)は、B細胞性腫瘍(英語版)の治療に用いられる抗がん剤である。経口投与可能な選択的不可逆的酵素阻害薬であり、ブルトン型チロシンキナーゼ(Bruton's tyrosine kinase; BTK)を阻害する。 リンパ球の一つであるB細胞に由来する悪性腫瘍である瀰漫性大細胞型B細胞性リンパ腫や多発性骨髄腫の治療に使用される。

効能

抗悪性腫瘍薬, ブルトン型チロシンキナーゼ阻害薬

商品名

イムブルビカ (ヤンセンファーマ)

説明

In November 2013, the US FDA approved ibrutinib (also referred to as PCI-32765), for the treatment of patients with mantle cell lymphoma (MCL) who had received at least one prior therapy. Ibrutinib is the second oral agent approved for the treatment of MCL. It works by irreversibly inhibiting Bruton’s tyrosine kinase (Btk) leading to the inhibition of B-cell receptor signaling and resulting in the reduction of malignant B-cell proliferation and induction of cell death. Btk plays an important role in the differentiation, development, proliferation, and survival of B cells via activation of cell-cycle regulators and regulating the expression of pro- and antiapoptotic proteins. Aberrant Btk activity results in a variety of B-cell malignancies including MCL. Ibrutinib inhibits Btk by irreversibly binding to cysteine-481 in the active site thereby inhibiting phosphorylation of tyrosine-223 and affecting downstream B-cell signaling pathways. Ibrutinib is a potent inhibitor of Btk (IC50=0.5 nM) and is efficacious in canine models of B-cell lymphoma. At dose ranges of 2.5–20 mg/kg, there was full occupancy of Btk in peripheral blood and tumor tissue for 24 h. A synthetic route to ibrutinib that employs Suzuki coupling of 3-iodo-1Hpyrazolo[3,4-d]pyrimidin-4-amine with (4-phenoxyphenyl)boronic acid followed by Mitsunobu reaction with N-Boc-3-hydroxypiperidine as key steps has been reported.

Originator

Celera/Pharmacyclics (United States)

定義

ChEBI: A member of the class of acrylamides that is (3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine in which the piperidine nitrogen is replaced by an acryloyl group. A selective and covalent inhibitor of he enzyme Bruton's tyrosine kinase, it is used for treatment of B-cell malignancies.

適応症

The collection of ibrutinib (Imbruvica(R), Pharmacyclics Inc.), afatinib, and osimertinib represents the small, yet expanding, group of covalent SMKIs. Ibrutinib is a non-receptor Bruton’s tyrosine kinase inhibitor approved for the treatment of relapsed chronic lymphocytic leukemia. Afatinib, approved for NSCLC in 2013 and squamous NSCLC in 2016, is a second-generation irreversible EGFR inhibitor that targets wild-type EGFR, the mutant T790M EGFR, and HER2. Osimertinib (AZD9291), which was approved by FDA in November 2015, is a third-generation irreversible EGFR inhibitor that selectively targets the mutant T790M EGFR. Rociletinib, which shares a high degree of structural similarity with that of osimertinib, is a promising covalent EGFR inhibitor developed by Clovis Oncology aimed for the treatment of patients with EGFR T790M-mutated NSCLC, until the company terminated its development in May 2016 following a negative vote fromthe FDA’sOncologic Drugs Advisory Committee.

brand name

Imbruvica

Chemical Synthesis

Condensation of commercially available 4-phenoxybenzoyl chloride (88) with malononitrile followed by acidic quench and O-methylation with dimethyl sulfate furnished vinyl dinitrile 89 in 84% yield over the three-step sequence. Next, treatment with hydrazine hydrate in refluxing ethanol secured aminopyrazole 90 and this was followed by treatment with neat formamide at elevated temperature to furnish pyrimidopyrazole 91 in excellent conversion. Selective alkylation of the pyrazole nitrogen with commercially- available (S)-piperidinyl tosylate (92) proceeded in 32% yield. Finally, liberation of the amide followed by pH adjustment and amide bond formation with acrolyl chloride furnished ibrutinib (XI) in 50% over the three-step sequence.

イブルチニブ 上流と下流の製品情報

原材料

準備製品


イブルチニブ 生産企業

Global( 442)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
010-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Hebei Jimi Trading Co., Ltd.
+86 319 5273535
bestoneforyou@sina.com CHINA 292 58
Shenzhen Excellent Biotech Co., Ltd.
13480692018
ramyan@ex-biotech.com;sale@ex-biotech.com CHINA 955 58
Handan Tongyi New Material Technology Co., Ltd
+8617330042575
ty003@handantongyi.com CHINA 339 58
Shenzhen Shengda Pharma Limited
+86-755-85269922
WeChat:shengdapharm sales@shengdapharm.com CHINA 304 58
AFINE CHEMICALS LIMITED
008657185134551
008657185134895 info@afinechem.com CHINA 15559 58
Hangzhou Huarong Pharm Co., Ltd.
+8613588754946 +86-571-86758373
0086-571-81131109 sales@huarongpharm.com CHINA 3149 58
Jiangsu Monade Biological Technology Co., Ltd.
+8613857751219
gao@mndbio.com CHINA 240 58
Capot Chemical Co.,Ltd.
+86(0)13336195806 +86-571-85586718
+86-571-85864795 sales@capotchem.com China 20012 60
Henan DaKen Chemical CO.,LTD.
+86-371-66670886
info@dakenchem.com China 20914 58

936563-96-1( イブルチニブ)キーワード:


  • 936563-96-1
  • According to Lu imatinib
  • PCI-32765
  • 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one
  • 2-Propen-1-one, 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-
  • IBRUTINIB (PCI-32765);PCI32765
  • (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo-[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-
  • PCI-32765 (Ibrutinib)
  • IBRUTINIB
  • Factory supply high quality Ibrutinib Cas 936563-96-1 with best price and fast delivery
  • CS-188
  • Ibrutinib (API)
  • N6-(2-Carboxyethyl) 
  • (R)-1-(3-(4-aMino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyriMidin-1-yl)piperidin-1-yl)prop-2-en-1-one
  • 1-[(3R)-3-[4-AMino-3-(4-phenoxyphenyl)pyrazolo[3, 4-d]pyriMidin-1-yl]piperidin-1-yl]prop-2-en-1-one
  • Ibrutinib (PCI-32765)
  • 1-{3-[4-AMino-3-(4-phenoxy-phenyl)-pyrazolo[3,4-d]pyriMidin-1-yl]-piperidin-1-yl}-propenone
  • 1-{3-[4-Amino-3-(4-phenoxy-phenyl)-pyrazolo[3,4-d]pyrimidin-1-yl]-piperidin-1-yl}-but-3-en-1-one
  • 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one Ibrutinib (PCI32765)
  • PCI-32765 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one
  • Ibrutinib, >=98%
  • Lbrutinib
  • 1-[3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3, 4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one
  • 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one (Ibrutinib)
  • Ibrutinib fandachem
  • According to lu for
  • Ibrutinib ISO 9001:2015 REACH
  • Ibrutinib acetate salt
  • 1-[3-[4-Amino-3-(4-phenoxyphenyl)-1-pyrazolo[3,4-d]pyrimidinyl]-1-piperidinyl]-2-propen-1-one
  • イブルチニブ
  • イブルチニブ
  • イブルチニブ (JAN)
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