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크리조티닙

크리조티닙
크리조티닙 구조식 이미지
카스 번호:
877399-52-5
한글명:
크리조티닙
동의어(한글):
크리조티닙
상품명:
Crizotinib
동의어(영문):
Xalkori;Crizotinib;PF 2341066;Crozotinib;PF-02341066;(R)-Crizotinib;Crizotinib, >=98%;PF-2341066/Crizotinib;PF-02341066 Crizotinib;Crizotinib (PF2341066)
CBNumber:
CB12473904
분자식:
C21H22Cl2FN5O
포뮬러 무게:
450.343
MOL 파일:
877399-52-5.mol

크리조티닙 속성

녹는점
192 °C
끓는 점
599.2±50.0 °C(Predicted)
밀도
1.47±0.1 g/cm3(Predicted)
저장 조건
room temp
물리적 상태
powder
산도 계수 (pKa)
9.81±0.10(Predicted)
색상
white to tan
CAS 데이터베이스
877399-52-5
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
안전지침서 24/25
유엔번호(UN No.) UN 3077 9 / PGIII
WGK 독일 3
위험 등급 IRRITANT
HS 번호 29333990
그림문자(GHS):
신호 어: Warning
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H317 알레르기성 피부 반응을 일으킬 수 있음 피부 과민성 물질 구분 1 경고 P261, P272, P280, P302+P352,P333+P313, P321, P363, P501
H319 눈에 심한 자극을 일으킴 심한 눈 손상 또는 자극성 물질 구분 2A 경고 P264, P280, P305+P351+P338,P337+P313P
H341 유전적인 결함을 일으킬 것으로 의심됨 (노출되어도 생식세포 유전독성을 일으키지 않는다는 결정적인 증거가 있는 노출경로가 있다면 노출경로 기재) 생식세포 변이원성 물질 구분 2 경고 P201,P202, P281, P308+P313, P405,P501
H400 수생생물에 매우 유독함 수생 환경유해성 물질 - 급성 구분 1 경고 P273, P391, P501
예방조치문구:
P273 환경으로 배출하지 마시오.
P280 보호장갑/보호의/보안경/안면보호구를 착용하시오.
P305+P351+P338 눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

크리조티닙 C화학적 특성, 용도, 생산

개요

In August 2011, the United States FDA approved crizotinib (PF- 02341066) for the treatment of anaplastic lymphoma kinase (ALK) rearranged non-small-cell lung cancer (NSCLC). Crizotinib is a dual ATP competitive inhibitor of tyrosine kinases c-MET (Mesenchymal-Epithelial Transition Factor) kinase (cellular IC50=8 nM) and ALK (cellular IC50=20 nM), both of which are important targets for cancer chemotherapy. When crizotinib was tested for selectivity versus other kinases it was found to have enzyme IC50's within 100-fold multiples of c-MET for 13 of the 120 kinases tested. In cellular assays, crizotinib was found to inhibit RON (recepteur d’origine nantais) kinase with a 10-fold selectivity window over c-MET.

화학적 성질

White Solid

Originator

Pfizer (United States)

용도

A potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). A potential antitumor agent.

용도

Crizotinib is a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). Crizotinib is a potential antitumor agent.

용도

PF-2341066 (Crizotinib) is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM, respectivley

정의

ChEBI: A 3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine that has R configuration at the chiral centre. The active enantiomer, it acts as a kinase inhibitor and is used for the treatment of patients wi h locally advanced or metastatic non-small cell lung cancer (NSCLC)

Indications

Crizotinib (Xalkori(R), Pfizer), approved in 2011, was the first approved inhibitor targeting anaplastic lymphoma kinase (ALK). ROS protooncogene 1-encoded kinase (ROS1) of the tyrosine kinase insulin receptor class and MET proto-oncogene-encoded kinase of the hepatocyte growth factor receptor (HGFR) class are other kinases targeted by crizotinib.When approved in 2011, crizotinib was the first drug specifically targeting NSCLC patients. However, resistance to crizotinib was usually observed in approximately 8 months after initial application and more than half of crizotinib-treated patients experienced gastrointestinal side effects. In 2016,crizotinib was additionally approved for ROS1-positive NSCLC by FDA.

상표명

Xalkori

크리조티닙 준비 용품 및 원자재

원자재

준비 용품


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