Regorafenib monohydrate
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Regorafenib monohydrate 속성
- 저장 조건
- 2-8°C
- 용해도
- ≥25.05 mg/mL in DMSO; insoluble in H2O
- 물리적 상태
- 고체
- 물리적 상태
- 단단한 모양
- 색상
- Light yellow to orange
- InChIKey
- ZOPOQLDXFHBOIH-UHFFFAOYSA-N
- SMILES
- O(C1C=CC(NC(=O)NC2C=CC(Cl)=C(C(F)(F)F)C=2)=C(F)C=1)C1=CC=NC(C(=O)NC)=C1.O
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
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신호 어: | Warning | |||||||||||||||||||||
유해·위험 문구: |
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예방조치문구: |
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Regorafenib monohydrate C화학적 특성, 용도, 생산
개요
Regorafenib monohydrate (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor with potent anti-tumour and anti-angiogenic activity. It is approved for the treatment of metastatic colorectal cancer, advanced gastrointestinal mesenchymal stromal tumours and hepatocellular carcinoma.Clinical Use
Regorafenib was approved by the U.S. Food and Drug Administration (FDA) in September 2012 for the treatment of metastatic colorectal cancer in patients who have previously undergone fluoropyrimidine-, oxaliplatin-, and irinotecan-based therapies. The FDA expanded the approved use of the drug to include patients with advanced gastrointestinal stromal tumors (GIST) that cannot be surgically removed and no longer respond to imatinib and sunitinib, two other drugs approved for treatment of GIST. Regorafenib, marketed under the trade name Stivarga®, was discovered and developed by Bayer Pharmaceuticals and marketed jointly with Onyx Pharmaceuticals. The active metabolites of the drug inhibit multiple targets within a variety of kinase families including those in the RET, VEGF, FGFR, PTK, and Abl pathways.Synthesis
Among several published synthesis, the most likely process scale synthesis will be highlighted from the two published syntheses, and this is described in the scheme. Commercially available picolinic acid (148) was heated with thionyl chloride to provide the crude intermediate 4-chloro-2- pyridyl acid chloride which was subsequently reacted with aqueous methyl amine in toluene to give 4- chloro-2-methylcarboxamide as its hydrochloride salt 149 in quantitative yield after treatment with acetyl chloride in toluene and ethanol. The hydrochloride salt was free based with sodium hydroxide and then immediately reacted with imine 150 (formed upon exposure to 4-amino-3-fluorophenol (153) in refluxing 3-methyl 2-butanone) in base to provide diaryl ether 151 in 84% yield. Reaction of amine 151 with the commercially available isocyanate 152 ultimately delivered regorafenib hydrate (XXIII) in 83% yield.Regorafenib monohydrate 준비 용품 및 원자재
원자재
준비 용품
Regorafenib monohydrate 공급 업체
글로벌( 247)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Yangzhou Qinyuan Pharmatech Co.,ltd | +86-18752526868 |
jennysun@yzqyyykj.com | China | 71 | 58 |
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. | +86-18600796368 +86-18600796368 |
sales@sjar-tech.com | China | 74 | 58 |
Hebei Yanxi Chemical Co., Ltd. | +86-17531190177; +8617531190177 |
peter@yan-xi.com | China | 6011 | 58 |
Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 |
sales@capotchem.com | China | 29798 | 60 |
Beijing Cooperate Pharmaceutical Co.,Ltd | 010-60279497 |
sales01@cooperate-pharm.com | CHINA | 1811 | 55 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21670 | 55 |
Nanjing ChemLin Chemical Industry Co., Ltd. | 025-83697070 |
product@chemlin.com.cn | CHINA | 3012 | 60 |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
ivan@atkchemical.com | China | 32760 | 60 |
Anqing Chico Pharmaceutical Co., Ltd. | 15380796838 |
chloewu@chicopharm.cn | CHINA | 341 | 58 |
career henan chemical co | +86-0371-86658258 +8613203830695 |
sales@coreychem.com | China | 29897 | 58 |
Regorafenib monohydrate 관련 검색:
4-아미노-3-플루오로페놀(4-아미노-3-플루오르페놀)
Alectinib Hydrochloride
PLX4032
Nintedanib Ethanesulfonate Salt
Olaparib
4-(4-AMINO-3-FLUOROPHENOXY)-N-METHYLPICOLINAMIDE
4-Chloro-alpha,alpha,alpha-trifluoro-m-toluidine
Regorafenib
Crizotinib
Afatinib (BIBW 2992)
PLERIXAFOR
Regorafenib (Hydrochloride)
SOLITHROMYCIN
Afatinib dimaleate
Dacomitinib (PF299804)
Cabozantinib Malate
918504-65-1
1110813-31-4