레고라페닙

한글명:레고라페닙

카스 번호755037-03-7

상품명:Regorafenib

CBNumberCB32498792

분자식C21H15ClF4N4O3

포뮬러 무게482.82

MOL 파일755037-03-7.mol

동의어(한글)

레고라페닙

화학적 성질

녹는점	206.0 to 210.0 °C
끓는 점	513.4±50.0 °C(Predicted)
밀도	1.491±0.06 g/cm3(Predicted)
저장 조건	Refrigerator
용해도	DMSO(약간 용해됨), 메탄올(약간 용해됨)
산도 계수 (pKa)	12.04±0.70(Predicted)
물리적 상태	백색 분말.
색상	옅은 핑크에서 라이트 핑크까지
CAS 데이터베이스	755037-03-7

위험 및 안전 성명

HS 번호

29242990

NFPA 704:

	0
2		0

그림문자(GHS)

레고라페닙 화학적 특성, 용도, 생산

개요
In September 2012, theUSFDAapproved regorafenib for the treatment of patients with metastatic colorectal cancer (CRC), especially those for whom standard therapies have failed, including fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, ananti-EGFRtherapy. Regorafenib is a multikinase inhibitor with potent inhibitory activity versus VEGFRs and PDFRs. Both of these classes of receptors are expressed on tumor cells and affect proliferation and angiogenesis. Regorafenib inhibited growth in murine xenograft models for colon, breast, renal, lung, melanoma, pancreatic, and ovarian tumors when dosed at 10–30 mg/kg. Regorafenib is a fluorinated analog of sorafenib, a multikinase inhibitor co-marketed by Bayer and Onyx for the treatment of kidney and liver cancer. The synthesis of regorafenib is accomplished in two steps from commercially available starting materials. 4-Aminophenol is coupled to 4-chloro-N-methyl- 2-pyridinecarboxamide to give 4-(2-(N-methylcarbamoyl)-4-pyridyloxy)aniline. Subsequent treatment with 4-chloro-3-(trifluoromethyl)phenyl isocycanate affords the urea, regorafenib.
Characteristics
Class: receptor tyrosine kinase
Treatment: colorectal cancer, GIST, HCC
Elimination half-life = 26-28 h
Protein binding = 99.5%
용도
BAY 73-4506 (Regorafenib) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf.
정의
ChEBI: A pyridinecarboxamide obtained by condensation of 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]pyridine-2-carboxylic acid with methylamine. Used for for the treatment of metastatic colorectal cancer in patients who have previ usly received chemotherapy, anti-EGFR or anti-VEGF therapy.

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