루카파립

루카파립
루카파립 구조식 이미지
카스 번호:
283173-50-2
한글명:
루카파립
동의어(한글):
루카파립
상품명:
Rucaparib
동의어(영문):
Rucaparib Base;8-fluoro-5-(4-((methylamino)methyl)phenyl)-2,3,4,6-tetrahydro-1H-azepino[5,4,3-cd]indol-1-one;Rikapbu;AG-14447;AG014447;Rucaparib;AG 014447;PF-01367388;AG 014447;AG014447;Rucaparib impurity
CBNumber:
CB51475507
분자식:
C19H18FN3O
포뮬러 무게:
323.36
MOL 파일:
283173-50-2.mol

루카파립 속성

녹는점
187 - 189°C
끓는 점
625.2±55.0 °C(Predicted)
밀도
1.281
저장 조건
2-8°C(protect from light)
용해도
DMSO(약간 용해됨), 메탄올(약간 용해됨)
물리적 상태
노란색 고체.
산도 계수 (pKa)
14.10±0.20(Predicted)
색상
연한 노란색에서 노란색까지
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
그림문자(GHS): GHS hazard pictograms
신호 어: Warning
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H361 태아 또는 생식능력에 손상을 일으킬 것으로 의심됨 생식독성 물질 구분 2 경고 P201, P202, P281, P308+P313, P405,P501
예방조치문구:
P201 사용 전 취급 설명서를 확보하시오.
P202 모든 안전 조치 문구를 읽고 이해하기 전에는 취급하지 마시오.
P281 요구되는 개인 보호구를 착용하시오
P308+P313 노출 또는 접촉이 우려되면 의학적인 조치· 조언를 구하시오.
P405 밀봉하여 저장하시오.
P501 ...에 내용물 / 용기를 폐기 하시오.

루카파립 C화학적 특성, 용도, 생산

개요

Rucaparib was approved in the US as an oral treatment for advanced ovarian cancer. Development of rucaparib began with collaborations between Cancer Research UK and Agouron Pharmaceuticals (later acquired by Pfizer). Global development rights for rucaparib were ultimately granted to Clovis Oncology via a licensing agreement from Pfizer. To qualify for treatment with rucaparib monotherapy, patients must demonstrate deleterious breast cancer (BRCA) mutation (germline and/or somatic)- associated advanced ovarian cancer and also must have previously been treated with two or more chemotherapy regimens. Rucaparib functions as a small molecule poly(ADPribose) polymerase (PARP) inhibitor, which plays an important role in DNA repair. This newly approved drug displays nanomolar potency against PARP-1, -2, and -3 enzymes, which translates into improved efficacy over alternative therapies such as olaparib or niraparib. Furthermore, rucaparib is also known to cause vasodilation, which is thought to induce tumor perfusion and increased accumulation of the drug in cancer cells. Although rucaparib shows higher cytotoxicity in cancer cells with mutation of BRCA1/2 genes and other DNA repair genes, reduced tumor growth was observed in mouse xenograft models of human cancers with and without BRCA mutations.Rucaparib is also being pursued as a treatment for breast cancer and has displayed promising initial results in trials for pancreatic cancer.

용도

Rucaparib is PARP1 inhibitor. It can be used in biological study of chemical screening to identify drugs that enhance or mitigate cellular responses to antibody-toxin fusion proteins using human B cell precursor leukemia cells and cervical adenocarcinoma cells.

루카파립 준비 용품 및 원자재

원자재

준비 용품


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