보수티닙

보수티닙
보수티닙 구조식 이미지
카스 번호:
380843-75-4
한글명:
보수티닙
동의어(한글):
보수티닙
상품명:
Bosutinib
동의어(영문):
CS-311;SKI-606;Bsutinib;Bosulif);BOSUTINIB;WAY-173606;Bosutinib CRS;Bosutinib-13CD3;Bosutinib control;Bosulif(bosutinib)
CBNumber:
CB6504575
분자식:
C26H29Cl2N5O3
포뮬러 무게:
530.45
MOL 파일:
380843-75-4.mol
MSDS 파일:
SDS

보수티닙 속성

녹는점
116-120 ºC
끓는 점
649.7±55.0 °C(Predicted)
밀도
1.36
증기압
0-0Pa at 20℃
저장 조건
room temp
용해도
DMSO: ≥15mg/mL
산도 계수 (pKa)
7.63±0.10(Predicted)
물리적 상태
가루
색상
황백색부터 연한 갈색까지
안정성
제공된 대로 구매일로부터 2년 동안 안정적입니다. DMSO의 솔루션은 -20°C에서 최대 1개월 동안 보관할 수 있습니다.
InChIKey
PICKMQXYAMDEPF-UHFFFAOYSA-N
LogP
3.3-4.3 at pH9.5
표면장력
72.4mN/m at 3.6mg/L and 20℃
CAS 데이터베이스
380843-75-4(CAS DataBase Reference)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 Xi
위험 카페고리 넘버 36
안전지침서 26
WGK 독일 3
HS 번호 29335990
그림문자(GHS): GHS hazard pictograms
신호 어: Warning
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H319 눈에 심한 자극을 일으킴 심한 눈 손상 또는 자극성 물질 구분 2A 경고 GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H413 장기적 영향에 의해 수생생물에 유해의 우려가 있음 수생 환경유해성 물질 - 만성 구분 4
예방조치문구:
P273 환경으로 배출하지 마시오.
P305+P351+P338 눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.
NFPA 704
0
2 0

보수티닙 C화학적 특성, 용도, 생산

개요

Bosutinib, similar to dasatinib, was developed as a dual inhibitor of the SCR family of kinases and the ABL kinase, thus applicable for Ph+ leukemias. In September 2012, the US FDA approved bosutinib (also referred to as SKI-607) for the treatment of relapsed or refractory chronicmyeloid leukemia (CML) for patients with resistance or intolerance to prior therapy.

화학적 성질

Pale Yellow Solid
Class: non-receptor tyrosine kinase
Treatment: CML
Oral bioavailability = 34%
Elimination half-life = 22.5 h
Protein binding = 95%

용도

Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM, respectively. It is built around a chemical scaffold that is different from that of imatinib. peripheral vasolidator increases cerebral blood flow, potential therapeutic for Altzheimer’s disease, cognitive impairment and dementia.

정의

ChEBI: Bosutinib is an aminoquinoline that is 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline bearing additional cyano and methoxy substituents at positions 3 and 6 respectively. It has a role as an antineoplastic agent and a tyrosine kinase inhibitor. It is a nitrile, a N-methylpiperazine, an aromatic ether, a tertiary amino compound, an aminoquinoline and a dichlorobenzene.

일반 설명

Bosutinib is a safe oral medicine with good bioavailability. It is effective for treating chronic myeloid leukemia (CML). It is also a potent ATP-competitive inhibitor for Src tyrosine kinase. Bosutinib inhibits epidermal growth factor receptor (EGFR). It suppresses solid tumors associated with breast, pancreas and prostate.

부작용

Possible side effects of bosutinib include Nausea, vomiting, stomach/abdominal pain, loss of appetite, cough, joint pain, headache, or dizziness may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly. Diarrhea is a common side effect.
www.webmd.com

target

BCR-ABL

Mode of action

Bosutinib is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl and Src kinases with potential antineoplastic activity. Unlike imatinib, bosutinib inhibits the autophosphorylation of both Abl and Src kinases, resulting in inhibition of cell growth and apoptosis. Because of the dual mechanism of action, this agent may have activity in resistant CML disease, other myeloid malignancies and solid tumors. Abl kinase is upregulated in the presence of the abnormal Bcr-abl fusion protein which is commonly associated with chronic myeloid leukemia (CML). Overexpression of specific Src kinases is also associated with the imatinib-resistant CML phenotype.

보수티닙 준비 용품 및 원자재

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