AZD-9291
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AZD-9291 속성
- 녹는점
- >188oC (dec.)
- 밀도
- 1.19±0.1 g/cm3(Predicted)
- 저장 조건
- Hygroscopic, -20°C Freezer, Under inert atmosphere
- 용해도
- DMSO (Slightly, Heated), Methanol (Slightly, Heated)
- 산도 계수 (pKa)
- 12.68±0.70(Predicted)
- 물리적 상태
- 고체
- 물리적 상태
- 단단한 모양
- 색상
- 연한 노란색~베이지색
- CAS 데이터베이스
- 1421373-65-0
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
HS 번호 | 29339900 |
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AZD-9291 C화학적 특성, 용도, 생산
개요
AZD-9291 (Mesylate), also known as Osimertinib, belongs to a third-generation EGFR (epidermal growth factor receptor) inhibitor. It can be used for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) in case when the cancer cells carry specific mutations (such as T790M) in the epidermal growth factor receptor. It takes effect through directly binding to the certain mutant forms of EGFR (T790M, L858R, and exon 19 deletions) that are frequently found in NSCLC, further causing poor prognosis for late-stage disease. Since it spares wild type EGFR during therapy, it has only limited toxicity.용도
AZD 9291 is an irreversible inhibitor of epidermal growth factor receptor (EGFR) sensitizing and T790M resistance mutations (IC50s = 15-17 nM) while sparing the wild-type form of the receptor (IC50 = 480 nM). It binds the related IGF1R and hERG receptors with significantly reduced potency (IC50s = 2.9 and 16.2 μM, respectively). AZD 9291 has been shown to inhibit tumor growth in a xenograft mouse model at oral doses of 5-10 mg/kg and has been tested clinically in patients with advanced EGFR mutant non-small-cell lung cancer.[Cayman Chemical]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 aminopyrimidines that is 4-(1-methylindol-3-yl)pyrimidin-2-amine in which one of the amino hydrogens is replaced by a 2-methoxy-4-[2-(dimethylamino)ethyl](methyl)amino-5-acrylamidophenyl group. Used (as the mesylate salt) for treat ent of EGFR T790M mutation positive non-small cell lung cancer.참고 문헌
http://www.medkoo.com/products/6711https://en.wikipedia.org/wiki/Osimertinib
https://www.drugbank.ca/drugs/DB09330
AZD-9291 준비 용품 및 원자재
원자재
Mutated EGFR-IN-1
3-chloro-N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-ylamino)phenyl)propanamid
아크릴일클로라이드
아크릴산
준비 용품
AZD-9291 공급 업체
글로벌( 373)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Hebei Mojin Biotechnology Co., Ltd | +86 13288715578 +8613288715578 |
sales@hbmojin.com | China | 12446 | 58 |
shandong perfect biotechnology co.ltd | +86-53169958659; +8618596095638 |
sales@sdperfect.com | China | 294 | 58 |
Henan Bao Enluo International TradeCo.,LTD | +86-17331933971 +86-17331933971 |
deasea125996@gmail.com | China | 2503 | 58 |
SHANDONG BOYUAN PHARMACEUTICAL CO., LTD. | +86-0531-69954981 +8615666777973 |
dwyane.wang@boyuanpharm.com | China | 211 | 58 |
Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 |
info@fdachem.com | China | 20293 | 58 |
Apeloa production Co.,Limited | +8619933239880 |
admin@apcl.com.cn | China | 853 | 58 |
Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 |
sales@capotchem.com | China | 29798 | 60 |
Shanghai Daken Advanced Materials Co.,Ltd | +86-371-66670886 |
info@dakenam.com | China | 18628 | 58 |
Nanjing Gold Pharmaceutical Technology Co. Ltd. | 025-84209270 15906146951 |
CHINA | 115 | 55 | |
Beijing Cooperate Pharmaceutical Co.,Ltd | 010-60279497 |
sales01@cooperate-pharm.com | CHINA | 1811 | 55 |
AZD-9291 관련 검색:
제니스테인
3-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[5,6-e]pyrimidin-7-yl]-N-methylbenzamide
Osimertinib dimesylate
Osimertinib mesylate
3,5-Dimethyl-4-methoxy-2-pyridinemethanol
N-(2-(dimethylamino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide
Olmutinib
XL-647
AZD 3759
AG 1478 HYDROCHLORIDE
OSI-420
Anlotinib
EGF816
Tucatinib
Neratinib
Poziotinib (HM781-36B)
Dacomitinib (PF299804)
Bortezomib