카보잔티닙

카보잔티닙 속성

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, respectively

정의

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/VEGFR

카보잔티닙 준비 용품 및 원자재

원자재

준비 용품

카보잔티닙 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	255	58
shandong perfect biotechnology co.ltd	+86-53169958659 +86-13153181156	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

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