ChemicalBook
Chinese English Japanese Germany Korea

Ibrutinib

Ibrutinib 구조식 이미지
카스 번호:
936563-96-1
상품명:
Ibrutinib
동의어(영문):
Lbrutinib;1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one;PCI-32765;Ibrutinib (PCI-32765);IBRUTINIB (PCI-32765);PCI32765;1-{3-[4-AMino-3-(4-phenoxy-phenyl)-pyrazolo[3,4-d]pyriMidin-1-yl]-piperidin-1-yl}-propenone;(R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo-[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-;(R)-1-(3-(4-aMino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyriMidin-1-yl)piperidin-1-yl)prop-2-en-1-one;CS-188;IBRUTINIB
CBNumber:
CB12515873
분자식:
C25H24N6O2
포뮬러 무게:
440.5
MOL 파일:
936563-96-1.mol

Ibrutinib 속성

녹는점
153-158°C
끓는 점
715.0±60.0 °C(Predicted)
밀도
1.34
저장 조건
-20°C
용해도
Soluble in DMSO ( up to at least 25 mg/ml)
물리적 상태
solid
산도 계수 (pKa)
4.09±0.30(Predicted)
색상
White or off-white
안정성
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
CAS 데이터베이스
936563-96-1

안전

유해 물질 데이터 936563-96-1(Hazardous Substances Data)

Ibrutinib C화학적 특성, 용도, 생산

개요

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.

용도

Ibrutinib is a highly selective Bruton’s tyrosine kinase (Btk) irreversible inhibitor.

Indications

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.

정의

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.

Ibrutinib 준비 용품 및 원자재

원자재

준비 용품


Ibrutinib 공급 업체

글로벌( 482)공급 업체
공급자 전화 이메일 국가 제품 수 이점
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
sales01@cooperate-pharm.com CHINA 1815 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 CHINA 955 58
Shenzhen Shengda Pharma Limited
755-85269922 +8613424394241
sales@shengdapharm.com CHINA 310 58
AFINE CHEMICALS LIMITED
0571-85134551
info@afinechem.com CHINA 15558 58
Hangzhou Huarong Pharm Co., Ltd.
571-86758373 +8613588754946
sales@huarongpharm.com CHINA 3149 58
Handan Tongyi New Material Technology Co., Ltd
+8617330042575
ty003@handantongyi.com China 378 58
Jiangsu Monade Biological Technology Co., Ltd.
+8613857751219
gao@mndbio.com CHINA 240 58
SyncoZymes (Shanghai) Co., Ltd.,
+8613681683526
lchen@syncozymes.com China 137 58
Qiuxian Baitai New Material Co., LTD
+8619932103556
larissa@qxbttech.com China 1691 58

Copyright 2019 © ChemicalBook. All rights reserved