카보잔티닙
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카보잔티닙 속성
- 녹는점
- 212-215°C
- 끓는 점
- 758.1±60.0 °C(Predicted)
- 밀도
- 1.396
- 저장 조건
- -20°C
- 용해도
- DMSO에 용해됨
- 물리적 상태
- 백색 분말.
- 산도 계수 (pKa)
- 13.86±0.70(Predicted)
- 색상
- 하얀색
- 안정성
- 제공된 대로 구매일로부터 1년 동안 안정적입니다. DMSO의 솔루션은 -20°C에서 최대 1개월 동안 보관할 수 있습니다.
- InChIKey
- ONIQOQHATWINJY-UHFFFAOYSA-N
- SMILES
- C1(C(NC2=CC=C(OC3C4C(N=CC=3)=CC(OC)=C(OC)C=4)C=C2)=O)(C(NC2=CC=C(F)C=C2)=O)CC1
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
카보잔티닙 C화학적 특성, 용도, 생산
개요
Cabozantinib was approved inNovember 2012 for the treatment of patients with progressive, unresectable, locally advanced, or metastatic medullary thyroid cancer (MTC). Cabozantinib was granted orphan drug status by the FDA to facilitate development of newtreatment options for patients with MTC. It is a member of a class of tyrosine kinase inhibitors (TKIs) with nanomolar pan-inhibitory activity against VEGFR2, MET, and RET among others. Inhibition of the VEGF pathway has been shown preclinically to initially slow tumor growth, but rapid revascularization is followed by aggressive tumor growth. The MET pathway has been implicated in the development of VEGF resistance, so dual VEGF/MET activity is viewed as desirable. In addition, mutations in RET play a particular role in MTC, with 25% of the tumors inheriting a germlinemutation in the proto-oncogene, so multiple tyrosine kinase inhibition may be viewed as particularly beneficial for the treatment of MTC.용도
Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively정의
ChEBI: A dicarboxylic acid diamide that is N-phenyl-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide in which the hydrogen at position 4 on the phenyl ring is substituted by a (6,7-dimethoxyquinolin-4-yl)oxy group. A multi-t rosine kinase inhibitor, used (as its malate salt) for the treatment of progressive, metastatic, medullary thyroid cancer.일반 설명
Class:receptor tyrosine kinase; Treatment: MTC; RCC; HCC; Other name: XL-184, BMS-907351; Elimination half-life = 110 h; Protein binding > 99.7%Clinical Use
Cabozantinib (PF-06463922; brand name Cabometyx; Exelixis, Alameda, CA) is an oral multikinase inhibitor with CNS penetration. It is FDA approved for use in medullary thyroid cancer and as a second-line agent in advanced renal cell carcinoma. In vitro studies found it to exhibit excellent activity against both the wild-type ROS1 fusion and the G2032R and G2026M mutations at concentrations less than 30?nmol/L—a dose much lower than what is clinically achievable [71, 91]. It has been found to inhibit CD74-ROS1-transformed Ba/F3 cells with more potency than entrectinib, brigatinib, lorlatinib [92], or foretinib [71].target
RET/VEGFR카보잔티닙 준비 용품 및 원자재
원자재
벤제나민,4-[(6,7-디메톡시-4-퀴놀리닐)옥시]-
1-(4-플루오로페닐카르바모일)시클로프로판카르복실산
Cabozantinib Malate
메틸1-[(4-플루오로페닐)카르바모일]시클로프로판카르복실레이트
준비 용품
카보잔티닙 공급 업체
글로벌( 426)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Shandong Risen-Sun Pharmaceutical Co., Ltd | +86-15552509998 +86-15621883869 |
liutf@jewim.com.cn | China | 251 | 58 |
Jinan Good Medical Technology Co.,Ltd | +86-53155562571 +86-008613553167512 |
13553167512@139.com | China | 23 | 58 |
HangZhou RunYan Pharma Technology Co.,LTD. | +8618882027439 |
sales2@runyanpharma.com | China | 302 | 58 |
SHANGHAI KEAN TECHNOLOGY CO., LTD. | +8613817748580 |
cooperation@kean-chem.com | China | 40066 | 58 |
Shanghai Joiny Pharmaceutical Co.,LTD | +8613681955282 |
gyd@joiny-pharma.com | China | 254 | 58 |
shandong perfect biotechnology co.ltd | +86-53169958659; +8618596095638 |
sales@sdperfect.com | China | 294 | 58 |
Apeloa production Co.,Limited | +8619933239880 |
admin@apcl.com.cn | China | 852 | 58 |
Capot Chemical Co.,Ltd. | +86-(0)57185586718 +86-13336195806 |
sales@capot.com | China | 29791 | 60 |
Nanjing Gold Pharmaceutical Technology Co. Ltd. | 025-84209270 15906146951 |
CHINA | 115 | 55 | |
Beijing Cooperate Pharmaceutical Co.,Ltd | 010-60279497 |
sales01@cooperate-pharm.com | CHINA | 1803 | 55 |