Ibrutinib
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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) |
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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 |
Ibrutinib 관련 검색:
Ibrutinib Impurity 25
Ibrutinib Impurity 28
Ibrutinib Dimer Impurity
(S)-3-Hydroxypiperidine
(S)-Ibrutinib
Ibrutinib-biotin
Troglitazone
Sofosbuvir
Baricitinib
Niraparib
Methyl 4-chloro-2-(N-methyl-N-phenylsulphonamide)benzoate
5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyriMidin-4-ylaMine
(S)-1-Boc-3-hydroxypiperidine
Bortezomib
ABT-199
Trametinib
N-(3-(5-(4-Chlorophenyl)-1H-pyrrolo[2,3-B]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonaMide
Erlotinib